MedKoo Cat#: 319830 | Name: Gosogliptin

Description:

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

Gosogliptin, also known as PF-734200 or PF-00734200, is a DPP-4 inhibitor under development for Type 2 diabetes mellitus.

Chemical Structure

Gosogliptin
Gosogliptin
CAS#869490-23-3 (free base)

Theoretical Analysis

MedKoo Cat#: 319830

Name: Gosogliptin

CAS#: 869490-23-3 (free base)

Chemical Formula: C17H24F2N6O

Exact Mass: 366.1980

Molecular Weight: 366.42

Elemental Analysis: C, 55.73; H, 6.60; F, 10.37; N, 22.94; O, 4.37

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Synonym
PF-734200; PF 734200; PF734200; PF-00734200; PF 00734200; PF00734200; Gosogliptin.
IUPAC/Chemical Name
(3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone
InChi Key
QWEWGXUTRTXFRF-KBPBESRZSA-N
InChi Code
InChI=1S/C17H24F2N6O/c18-17(19)2-5-25(12-17)15(26)14-10-13(11-22-14)23-6-8-24(9-7-23)16-20-3-1-4-21-16/h1,3-4,13-14,22H,2,5-12H2/t13-,14-/m0/s1
SMILES Code
O=C(N1CC(F)(F)CC1)[C@H]2NC[C@@H](N3CCN(C4=NC=CC=N4)CC3)C2
Appearance
Solid powder
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
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Related CAS# CAS No. 869490-23-3 (Gosogliptin) 869490-47-1 (Gosogliptin Hydrochloride
Product Data
Biological target:
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
Soluble in DMSO, not in water 0.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 366.42 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:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Sharma R, Sun H, Piotrowski DW, Ryder TF, Doran SD, Dai H, Prakash C. Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrol idin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. Drug Metab Dispos. 2012 Nov;40(11):2143-61. doi: 10.1124/dmd.112.047316. Epub 2012 Aug 15. PubMed PMID: 22896728. 2: Muto C, Dai H, Teeter JG, Johnson S, Cropp AB, Chiba K, Suwa T. The pharmacokinetics and pharmacodynamics of PF-00734200, a DPP-IV inhibitor, in healthy Japanese subjects. Int J Clin Pharmacol Ther. 2012 Jul;50(7):505-9. doi: 10.5414/CP201614. PubMed PMID: 22541754. 3: Terra SG, Somayaji V, Schwartz S, Lewin AJ, Teeter JG, Dai H, Nguyen TT, Calle RA. A Dose-Ranging Study of the DPP-IV Inhibitor PF-734200 Added to Metformin in Subjects With Type 2 Diabetes*. Exp Clin Endocrinol Diabetes. 2011 Jul;119(7):401-7. doi: 10.1055/s-0031-1273737. Epub 2011 Apr 6. PubMed PMID: 21472661. 4: Rosenstock J, Lewin AJ, Norwood P, Somayaji V, Nguyen TT, Teeter JG, Johnson SL, Dai H, Terra SG. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor PF-734200 added to metformin in Type 2 diabetes. Diabet Med. 2011 Apr;28(4):464-9. doi: 10.1111/j.1464-5491.2010.03181.x. PubMed PMID: 21392067. 5: Dai H, Johnson SL, Terra SG, Marbury TC, Smith WB, Alcorn H, Boyd RA, Wang R, Nguyen TT. The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency. Br J Clin Pharmacol. 2011 Jul;72(1):85-91. doi: 10.1111/j.1365-2125.2011.03954.x. PubMed PMID: 21366665; PubMed Central PMCID: PMC3141189. 6: Schwartz SL. Treatment of elderly patients with type 2 diabetes mellitus: a systematic review of the benefits and risks of dipeptidyl peptidase-4 inhibitors. Am J Geriatr Pharmacother. 2010 Oct;8(5):405-18. doi: 10.1016/j.amjopharm.2010.10.003. Review. PubMed PMID: 21335294. 7: Gustavson SM, Dai H, Preston GM, Somayaji V, Hirshberg B, Calle RA. Effects of multiple doses of the DPP-IV inhibitor PF-734200 on the relationship between GLP-1 and glucose in subjects with type 2 diabetes mellitus. Diabetes Res Clin Pract. 2011 Feb;91(2):e45-9. doi: 10.1016/j.diabres.2010.10.018. Epub 2010 Dec 4. PubMed PMID: 21130513. 8: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Nov;31(9):597-633. PubMed PMID: 20094643.