MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 333103 | Name: Tirzepatide

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Tirzepatide, also known as LY 3298176, is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Tirzepatide has a greater affinity to GIP receptors than to GLP-1 receptors, and this dual agonist behavior has been shown to produce greater reductions of hyperglycemia compared to a selective GLP-1 receptor agonist. Signaling studies reported that tirzepatide mimics the actions of natural GIP at the GIP receptor. Tirzepatide was approved for improving blood sugar control in adults with type 2 diabetes, as an addition to diet and exercise.

Chemical Structure

Tirzepatide
CAS#2023788-19-2

Theoretical Analysis

MedKoo Cat#: 333103

Name: Tirzepatide

CAS#: 2023788-19-2

Chemical Formula: C225H348N48O68

Exact Mass: 4810.5249

Molecular Weight: 4813.53

Elemental Analysis: C, 56.14; H, 7.29; N, 13.97; O, 22.60

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
BG 121; BG-121; BG121; LY 3298176; LY3298176; LY-3298176; Tirzepatide;
IUPAC/Chemical Name
L-Serinamide, L-tyrosyl-2-methylalanyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methylalanyl-L-leucyl-L-α-aspartyl-L-lysyl-L-isoleucyl-L-alanyl-L-glutaminyl-N6-[(22S)-22,42-dicarboxy-1,10,19,24-tetraoxo-3,6,12,15-tetraoxa-9,18,23-triazadotetracont-1-yl]-L-lysyl-L-alanyl-L-phenylalanyl-L-valyl-L-glutaminyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-alanylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-
InChi Key
BTSOGEDATSQOAF-MCNPHUAVSA-N
InChi Code
InChI=1S/C225H348N48O68/c1-23-126(10)183(264-198(311)146(64-50-52-88-226)246-202(315)157(109-180(297)298)252-199(312)152(103-124(6)7)261-223(337)225(21,22)269-217(330)185(128(12)25-3)266-209(322)163(120-278)257-200(313)153(107-138-74-78-141(282)79-75-138)250-203(316)158(110-181(299)300)253-207(320)162(119-277)259-216(329)187(134(18)280)267-206(319)155(106-136-60-44-41-45-61-136)254-215(328)186(133(17)279)262-174(289)114-237-193(306)147(83-87-179(295)296)260-222(336)224(19,20)268-192(305)143(227)104-137-72-76-140(281)77-73-137)214(327)242-131(15)190(303)244-148(80-84-168(228)283)196(309)245-145(65-51-53-89-231-175(290)121-340-100-99-339-97-91-233-176(291)122-341-101-98-338-96-90-232-170(285)86-82-150(221(334)335)243-171(286)70-46-38-36-34-32-30-28-26-27-29-31-33-35-37-39-47-71-178(293)294)195(308)240-130(14)191(304)248-154(105-135-58-42-40-43-59-135)205(318)263-182(125(8)9)212(325)247-149(81-85-169(229)284)197(310)251-156(108-139-111-234-144-63-49-48-62-142(139)144)201(314)249-151(102-123(4)5)204(317)265-184(127(11)24-2)213(326)241-129(13)189(302)236-112-172(287)235-115-177(292)270-92-54-66-164(270)210(323)258-161(118-276)208(321)256-160(117-275)194(307)238-113-173(288)239-132(16)218(331)272-94-56-68-166(272)220(333)273-95-57-69-167(273)219(332)271-93-55-67-165(271)211(324)255-159(116-274)188(230)301/h40-45,48-49,58-63,72-79,111,123-134,143,145-167,182-187,234,274-282H,23-39,46-47,50-57,64-71,80-110,112-122,226-227H2,1-22H3,(H2,228,283)(H2,229,284)(H2,230,301)(H,231,290)(H,232,285)(H,233,291)(H,235,287)(H,236,302)(H,237,306)(H,238,307)(H,239,288)(H,240,308)(H,241,326)(H,242,327)(H,243,286)(H,244,303)(H,245,309)(H,246,315)(H,247,325)(H,248,304)(H,249,314)(H,250,316)(H,251,310)(H,252,312)(H,253,320)(H,254,328)(H,255,324)(H,256,321)(H,257,313)(H,258,323)(H,259,329)(H,260,336)(H,261,337)(H,262,289)(H,263,318)(H,264,311)(H,265,317)(H,266,322)(H,267,319)(H,268,305)(H,269,330)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,334,335)/t126-,127-,128-,129-,130-,131-,132-,133+,134+,143-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-,182-,183-,184-,185-,186-,187-/m0/s1
SMILES Code
OC[C@@H](C(N)=O)NC([C@H]1N(C([C@H]2N(C([C@H]3N(C([C@H](C)NC(CNC([C@H](CO)NC([C@H](CO)NC([C@H]4N(C(CNC(CNC([C@H](C)NC([C@H]([C@@H](C)CC)NC([C@H](CC(C)C)NC([C@H](CC5=CNC6=C5C=CC=C6)NC([C@H](CCC(N)=O)NC([C@H](C(C)C)NC([C@H](CC7=CC=CC=C7)NC([C@H](C)NC([C@H](CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)NC([C@H](CCC(N)=O)NC([C@H](C)NC([C@H]([C@@H](C)CC)NC([C@H](CCCCN)NC([C@H](CC(O)=O)NC([C@H](CC(C)C)NC(C(C)(C)NC([C@H]([C@@H](C)CC)NC([C@H](CO)NC([C@H](CC8=CC=C(O)C=C8)NC([C@H](CC(O)=O)NC([C@H](CO)NC([C@H]([C@H](O)C)NC([C@H](CC9=CC=CC=C9)NC([C@H]([C@H](O)C)NC(CNC([C@H](CCC(O)=O)NC(C(C)(C)NC([C@H](CC%10=CC=C(O)C=C%10)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC4)=O)=O)=O)=O)=O)CCC3)=O)CCC2)=O)CCC1)=O
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
irzepatide is a newly developed glucose-lowering agent which acts on the glucose-dependent insulinotropic peptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. It has been shown to result in several highly beneficial outcomes including weight loss and a significant improvement in important metabolic parameters such as HbA1c, fasting serum glucose, and triglyceride/lipoprotein levels. These findings suggest that tirzepatide could potentially be beneficial to metabolically healthy obese or metabolically healthy overweight patients in reducing their risk of adverse cardiovascular outcomes and conversion to the metabolically unhealthy phenotype.
Biological target:
Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.
In vitro activity:
In mouse islets, tirzepatide stimulates insulin secretion predominantly through the GLP-1R. However, in human islets, antagonizing GIPR activity consistently decreases the insulin response to tirzepatide. Tirzepatide stimulates islet hormone secretion from human islets through both incretin receptors. Reference: Nat Metab. 2023 Jun;5(6):945-954. https://pubmed.ncbi.nlm.nih.gov/37277609/
In vivo activity:
As monotherapy for early type 2 diabetes, tirzepatide achieved significant improvements in biomarkers of both pancreatic beta-cell function and insulin sensitivity. Reference: J Endocr Soc. 2023 Apr 22;7(5):bvad056. https://pubmed.ncbi.nlm.nih.gov/37153701/

Preparing Stock Solutions

The following data is based on the product molecular weight 4,813.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. El K, Douros JD, Willard FS, Novikoff A, Sargsyan A, Perez-Tilve D, Wainscott DB, Yang B, Chen A, Wothe D, Coupland C, Tschöp MH, Finan B, D'Alessio DA, Sloop KW, Müller TD, Campbell JE. The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets. Nat Metab. 2023 Jun;5(6):945-954. doi: 10.1038/s42255-023-00811-0. Epub 2023 Jun 5. PMID: 37277609; PMCID: PMC10290954. 2. Lee CJ, Mao H, Thieu VT, Landó LF, Thomas MK. Tirzepatide as Monotherapy Improved Markers of Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes (SURPASS-1). J Endocr Soc. 2023 Apr 22;7(5):bvad056. doi: 10.1210/jendso/bvad056. PMID: 37153701; PMCID: PMC10157777. 3. Heise T, DeVries JH, Urva S, Li J, Pratt EJ, Thomas MK, Mather KJ, Karanikas CA, Dunn J, Haupt A, Milicevic Z, Coskun T. Tirzepatide Reduces Appetite, Energy Intake, and Fat Mass in People With Type 2 Diabetes. Diabetes Care. 2023 May 1;46(5):998-1004. doi: 10.2337/dc22-1710. PMID: 36857477; PMCID: PMC10154650.
In vitro protocol:
1. El K, Douros JD, Willard FS, Novikoff A, Sargsyan A, Perez-Tilve D, Wainscott DB, Yang B, Chen A, Wothe D, Coupland C, Tschöp MH, Finan B, D'Alessio DA, Sloop KW, Müller TD, Campbell JE. The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets. Nat Metab. 2023 Jun;5(6):945-954. doi: 10.1038/s42255-023-00811-0. Epub 2023 Jun 5. PMID: 37277609; PMCID: PMC10290954.
In vivo protocol:
1. Lee CJ, Mao H, Thieu VT, Landó LF, Thomas MK. Tirzepatide as Monotherapy Improved Markers of Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes (SURPASS-1). J Endocr Soc. 2023 Apr 22;7(5):bvad056. doi: 10.1210/jendso/bvad056. PMID: 37153701; PMCID: PMC10157777. 2. Heise T, DeVries JH, Urva S, Li J, Pratt EJ, Thomas MK, Mather KJ, Karanikas CA, Dunn J, Haupt A, Milicevic Z, Coskun T. Tirzepatide Reduces Appetite, Energy Intake, and Fat Mass in People With Type 2 Diabetes. Diabetes Care. 2023 May 1;46(5):998-1004. doi: 10.2337/dc22-1710. PMID: 36857477; PMCID: PMC10154650.
1: Stretton B, Kovoor J, Bacchi S, Chang S, Ngoi B, Murray T, Bristow TC, Heng J, Gupta A, Ovenden C, Maddern G, Thompson CH, Heilbronn L, Boyd M, Rayner C, Talley NJ, Horowtiz M. Weight Loss With Subcutaneous Semaglutide Versus Other Glucagon Like Peptide-1 Receptor Agonists In Type 2 Diabetes: A Systematic Review. Intern Med J. 2023 May 15. doi: 10.1111/imj.16126. Epub ahead of print. PMID: 37189293. 2: Copur S, Tanriover C, Yavuz F, Tuttle KR, Kanbay M. Tirzepatide and potential use for metabolically healthy obesity. Eur J Intern Med. 2023 May 12:S0953-6205(23)00164-4. doi: 10.1016/j.ejim.2023.05.012. Epub ahead of print. PMID: 37183081. 3: Perry D, Moe SS, Thomas B, Lindblad AJ, Kirkwood J, Falk J, Potter J, Paige A, Allan GM. Top studies of 2022 relevant to primary care: From the PEER team. Can Fam Physician. 2023 May;69(5):325-329. doi: 10.46747/cfp.6905325. PMID: 37172982; PMCID: PMC10177638. 4: Tamargo J, Agewall S, Borghi C, Ceconi C, Cerbai E, Dan GA, Ferdinandy P, Grove EL, Rocca B, Sulzgruber P, Semb AG, Sossalla S, Niessner A, Kaski JC, Dobrev D. New pharmacological agents and novel cardiovascular pharmacotherapy strategies in 2022. Eur Heart J Cardiovasc Pharmacother. 2023 May 11:pvad034. doi: 10.1093/ehjcvp/pvad034. Epub ahead of print. PMID: 37169875. 5: Lee CJ, Mao H, Thieu VT, Landó LF, Thomas MK. Tirzepatide as Monotherapy Improved Markers of Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes (SURPASS-1). J Endocr Soc. 2023 Apr 22;7(5):bvad056. doi: 10.1210/jendso/bvad056. PMID: 37153701; PMCID: PMC10157777. 6: Bosch C, Carriazo S, Soler MJ, Ortiz A, Fernandez-Fernandez B. Tirzepatide and prevention of chronic kidney disease. Clin Kidney J. 2022 Dec 23;16(5):797-808. doi: 10.1093/ckj/sfac274. PMID: 37151412; PMCID: PMC10157759. 7: Lin F, Yu B, Ling B, Lv G, Shang H, Zhao X, Jie X, Chen J, Li Y. Weight loss efficiency and safety of tirzepatide: A Systematic review. PLoS One. 2023 May 4;18(5):e0285197. doi: 10.1371/journal.pone.0285197. PMID: 37141329; PMCID: PMC10159347. 8: Bitsi S, El Eid L, Manchanda Y, Oqua AI, Mohamed N, Hansen B, Suba K, Rutter GA, Salem V, Jones B, Tomas A. Divergent acute versus prolonged pharmacological GLP-1R responses in adult β cell-specific β-arrestin 2 knockout mice. Sci Adv. 2023 May 3;9(18):eadf7737. doi: 10.1126/sciadv.adf7737. Epub 2023 May 3. PMID: 37134170; PMCID: PMC10156113. 9: Tirzepatide: A Dual Glucose-Dependent Insulinotropic Polypeptide and Glucagon-Like Peptide-1 Agonist for the Management of Type 2 Diabetes Mellitus: Erratum. Am J Ther. 2023 Apr 28. doi: 10.1097/MJT.0000000000001634. Epub ahead of print. PMID: 37126800. 10: Ma Z, Jin K, Yue M, Chen X, Chen J. Research Progress on the GIP/GLP-1 Receptor Coagonist Tirzepatide, a Rising Star in Type 2 Diabetes. J Diabetes Res. 2023 Apr 15;2023:5891532. doi: 10.1155/2023/5891532. PMID: 37096236; PMCID: PMC10122586. 11: Kushner P, Anderson JE, Simon J, Boye KS, Ranta K, Torcello-Gómez A, Levine JA. Efficacy and Safety of Tirzepatide in Adults With Type 2 Diabetes: A Perspective for Primary Care Providers. Clin Diabetes. 2023 Spring;41(2):258-272. doi: 10.2337/cd22-0029. Epub 2023 Nov 29. PMID: 37092144; PMCID: PMC10115620. 12: Gómez Lumbreras A, Tan MS, Villa-Zapata L, Ilham S, Earl JC, Malone DC. Cost-effectiveness analysis of five anti-obesity medications from a US payer's perspective. Nutr Metab Cardiovasc Dis. 2023 Jun;33(6):1268-1276. doi: 10.1016/j.numecd.2023.03.012. Epub 2023 Mar 25. PMID: 37088648. 13: Doggrell SA. Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? Expert Opin Investig Drugs. 2023 Apr 24:1-5. doi: 10.1080/13543784.2023.2206560. Epub ahead of print. PMID: 37086147. 14: Krauss Z, Hintz A, Fisk B. Tirzepatide: Clinical review of the "twincretin" injectable. Am J Health Syst Pharm. 2023 Apr 18:zxad080. doi: 10.1093/ajhp/zxad080. Epub ahead of print. PMID: 37070418. 15: Blüher M, Aras M, Aronne LJ, Batterham RL, Giorgino F, Ji L, Pietiläinen KH, Schnell O, Tonchevska E, Wilding JPH. New insights into the treatment of obesity. Diabetes Obes Metab. 2023 Apr 13. doi: 10.1111/dom.15077. Epub ahead of print. PMID: 37055715. 16: Meng Z, Yang M, Wen H, Zhou S, Xiong C, Wang Y. A systematic review of the safety of tirzepatide-a new dual GLP1 and GIP agonist - is its safety profile acceptable? Front Endocrinol (Lausanne). 2023 Mar 27;14:1121387. doi: 10.3389/fendo.2023.1121387. PMID: 37051199; PMCID: PMC10084319. 17: Copur S, Demiray A, Cherney D, Tuttle K, Kanbay M. Tirzepatide decreases systolic and diastolic blood pressure. Eur J Intern Med. 2023 Apr 10:S0953-6205(23)00121-8. doi: 10.1016/j.ejim.2023.04.005. Epub ahead of print. PMID: 37045710. 18: Shi Q, Nong K, Vandvik PO, Guyatt GH, Schnell O, Rydén L, Marx N, Brosius FC 3rd, Mustafa RA, Agarwal A, Zou X, Mao Y, Asadollahifar A, Chowdhury SR, Zhai C, Gupta S, Gao Y, Lima JP, Numata K, Qiao Z, Fan Q, Yang Q, Jin Y, Ge L, Yang Q, Zhu H, Yang F, Chen Z, Lu X, He S, Chen X, Lyu X, An X, Chen Y, Hao Q, Standl E, Siemieniuk R, Agoritsas T, Tian H, Li S. Benefits and harms of drug treatment for type 2 diabetes: systematic review and network meta-analysis of randomised controlled trials. BMJ. 2023 Apr 6;381:e074068. doi: 10.1136/bmj-2022-074068. PMID: 37024129; PMCID: PMC10077111. 19: Viljoen A, Pantalone KM, Galindo RJ, Cui X, Huh R, Hemmingway A, Fernández Landó L, Patel H. Time to Reach Glycaemic and Body Weight Loss Thresholds with Tirzepatide in Patients with Type 2 Diabetes: A Pre-planned Exploratory Analysis of SURPASS-2 and SURPASS-3. Diabetes Ther. 2023 May;14(5):925-936. doi: 10.1007/s13300-023-01398-1. Epub 2023 Mar 31. PMID: 37000390; PMCID: PMC10126190. 20: Chakhtoura M, Haber R, Ghezzawi M, Rhayem C, Tcheroyan R, Mantzoros CS. Pharmacotherapy of obesity: an update on the available medications and drugs under investigation. EClinicalMedicine. 2023 Mar 20;58:101882. doi: 10.1016/j.eclinm.2023.101882. PMID: 36992862; PMCID: PMC10041469.