Ketorolac tromethamine | CAS#74103-07-4 | NSAID inhibitor | COX-1/2 inhibitor

MedKoo Cat#: 540259 | Name: Ketorolac tromethamine

Description:

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

Ketorolac tromethamine is an NSAID and COX-1/2 inhibitor. It also prevents spinal injury-induced increase of PAR1 and decreases expression of PDE4D.

Chemical Structure

Ketorolac tromethamine

CAS#74103-07-4

Theoretical Analysis

MedKoo Cat#: 540259

Name: Ketorolac tromethamine

CAS#: 74103-07-4

Chemical Formula: C26H28FN3O9

Exact Mass: 376.1634

Molecular Weight: 376.41

Elemental Analysis: C, 57.25; H, 5.17; F, 3.48; N, 7.70; O, 26.40

Price and Availability

Size	Price	Availability
1g	USD 250.00	2 Weeks
5g	USD 550.00	2 Weeks
10g	USD 850.00	2 Weeks
25g	USD 1,450.00	2 Weeks

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Related CAS #

74103-07-4 66635-93-6 (R-isomer)

Synonym

Acular; Godek; Sprix; Syntex; Toradol; Ketorolac tromethamine

IUPAC/Chemical Name

2-amino-2-(hydroxymethyl)propane-1,3-diol 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylate

InChi Key

BWHLPLXXIDYSNW-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H13NO3.C4H11NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13;5-4(1-6,2-7)3-8/h1-7,11H,8-9H2,(H,18,19);6-8H,1-3,5H2

SMILES Code

O=C(C1C2=CC=C(C(C3=CC=CC=C3)=O)N2CC1)O.OCC(CO)(N)CO

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

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Ketorolac tromethamine salt (RS37619 tromethamine salt) is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.

In vitro activity:

KT promoted the proliferation of IL-1β-induced ATDC5 cells, whereas COX-2 overexpression reversed the promotive effects of KT, revealing that KT could alleviate IL-1β-induced chondrocyte injury by suppressing COX-2 expression. Reference: Exp Ther Med. 2022 May;23(5):337. https://pubmed.ncbi.nlm.nih.gov/35411209/

In vivo activity:

According to the anti-hyperagesia and anti-inflammation tests, which were used to determine the change in the pain threshold, NFR and swelling showed that the rat group given the phonophoretic transdermal delivery of KT (ketorolac tromethamine) exhibited significantly more noticeable anti-hyperalgesic and anti-inflammatory effects than those treated with the simple application of a KT gel. Reference: Arch Pharm Res. 2008 Apr;31(4):511-7. https://pubmed.ncbi.nlm.nih.gov/18449510/

	Solvent	mg/mL	mM
Solubility
	Ethanol	8.0	21.25
	Water	87.5	232.46

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 376.41 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.

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. Liu C, Chen Y. Ketorolac tromethamine alleviates IL-1β-induced chondrocyte injury by inhibiting COX-2 expression. Exp Ther Med. 2022 May;23(5):337. doi: 10.3892/etm.2022.11267. Epub 2022 Mar 18. PMID: 35411209; PMCID: PMC8992376. 2. Zhang W, Mei R, Wu S. Ketorolac tromethamine represses senescence in aging articular chondrocytes. Biosci Biotechnol Biochem. 2022 Jun 25;86(7):837-845. doi: 10.1093/bbb/zbac047. PMID: 35404445. 3. Yang JH, Kim TY, Lee JH, Yoon SW, Yang KH, Shin SC. Anti-hyperalgesic and anti-inflammatory effects of ketorolac tromethamine gel using pulsed ultrasound in inflamed rats. Arch Pharm Res. 2008 Apr;31(4):511-7. doi: 10.1007/s12272-001-1186-5. Epub 2008 May 1. PMID: 18449510.

In vitro protocol:

In vivo protocol:

1. Yang JH, Kim TY, Lee JH, Yoon SW, Yang KH, Shin SC. Anti-hyperalgesic and anti-inflammatory effects of ketorolac tromethamine gel using pulsed ultrasound in inflamed rats. Arch Pharm Res. 2008 Apr;31(4):511-7. doi: 10.1007/s12272-001-1186-5. Epub 2008 May 1. PMID: 18449510.

1: Li C, Li C, Liu Z, Li Q, Yan X, Liu Y, Lu W. Enhancement in bioavailability of ketorolac tromethamine via intranasal in situ hydrogel based on poloxamer 407 and carrageenan. Int J Pharm. 2014 Oct 20;474(1-2):123-33. doi: 10.1016/j.ijpharm.2014.08.023. Epub 2014 Aug 17. PubMed PMID: 25138250. 2: Vadivelu N, Gowda AM, Urman RD, Jolly S, Kodumudi V, Maria M, Taylor R Jr, Pergolizzi JV Jr. Ketorolac tromethamine - routes and clinical implications. Pain Pract. 2015 Feb;15(2):175-93. doi: 10.1111/papr.12198. Epub 2014 Apr 16. Review. PubMed PMID: 24738596. 3: Ticly FG, Lira RP, Zanetti FR, Machado MC, Rodrigues GB, Arieta CE. Prophylactic use of ketorolac tromethamine in cataract surgery: a randomized trial. J Ocul Pharmacol Ther. 2014 Aug;30(6):495-501. doi: 10.1089/jop.2013.0214. Epub 2014 Apr 15. PubMed PMID: 24735005. 4: Beitzel K, McCarthy MB, Cote MP, Apostolakos J, Russell RP, Bradley J, ElAttrache NS, Romeo AA, Arciero RA, Mazzocca AD. The effect of ketorolac tromethamine, methylprednisolone, and platelet-rich plasma on human chondrocyte and tenocyte viability. Arthroscopy. 2013 Jul;29(7):1164-74. doi: 10.1016/j.arthro.2013.04.006. PubMed PMID: 23809450. 5: Lyra AF, Bastos LC, Lima RC, Maranhão Lde V, Arantes TE. Artificial tears alone versus 0.45% ketorolac tromethamine with artificial tears for the treatment of acute viral conjunctivitis. Arq Bras Oftalmol. 2014 Apr;77(2):99-102. PubMed PMID: 25076474. 6: Mettu SR, Veerareddy PR. Formulation and pharmacokinetics of ketorolac tromethamine fast dissolving tablets. Drug Res (Stuttg). 2013 Nov;63(11):586-90. doi: 10.1055/s-0033-1348258. Epub 2013 Jun 18. PubMed PMID: 23780501. 7: Kalariya PD, Raju B, Borkar RM, Namdev D, Gananadhamu S, Nandekar PP, Sangamwar AT, Srinivas R. Characterization of forced degradation products of ketorolac tromethamine using LC/ESI/Q/TOF/MS/MS and in silico toxicity prediction. J Mass Spectrom. 2014 May;49(5):380-91. doi: 10.1002/jms.3351. PubMed PMID: 24809899. 8: Li X, Du L, Chen X, Ge P, Wang Y, Fu Y, Sun H, Jiang Q, Jin Y. Nasal delivery of analgesic ketorolac tromethamine thermo- and ion-sensitive in situ hydrogels. Int J Pharm. 2015 Jul 15;489(1-2):252-60. doi: 10.1016/j.ijpharm.2015.05.009. Epub 2015 May 6. PubMed PMID: 25957699. 9: Bullingham R, Juan A. Comparison of intranasal ketorolac tromethamine pharmacokinetics in younger and older adults. Drugs Aging. 2012 Nov;29(11):899-904. doi: 10.1007/s40266-012-0023-2. PubMed PMID: 23143939. 10: Stephens DM, Richards BG, Schleicher WF, Zins JE, Langstein HN. Is ketorolac safe to use in plastic surgery? A critical review. Aesthet Surg J. 2015 May;35(4):462-6. doi: 10.1093/asj/sjv005. Epub 2015 Mar 29. Review. PubMed PMID: 25825424. 11: Vemula SK. Formulation and pharmacokinetics of colon-specific double-compression coated mini-tablets: Chronopharmaceutical delivery of ketorolac tromethamine. Int J Pharm. 2015 Aug 1;491(1-2):35-41. doi: 10.1016/j.ijpharm.2015.06.007. Epub 2015 Jun 6. PubMed PMID: 26056929. 12: Vemula SK, Veerareddy PR. Development, evaluation and pharmacokinetics of time-dependent ketorolac tromethamine tablets. Expert Opin Drug Deliv. 2013 Jan;10(1):33-45. doi: 10.1517/17425247.2013.743528. Epub 2012 Nov 30. PubMed PMID: 23199134. 13: Kulo A, Hendrickx S, de Hoon J, Mulabegovic N, van Calsteren K, Verbesselt R, Allegaert K. The impact of pregnancy on urinary ketorolac metabolites after single intravenous bolus. Eur J Drug Metab Pharmacokinet. 2013 Mar;38(1):1-4. doi: 10.1007/s13318-012-0108-7. Epub 2012 Nov 21. PubMed PMID: 23179562. 14: Mathew ST, Subbiah GD, Vasantha PV, Balan V. Characterization and pharmacokinetic evaluation of gamma sterilized ketorolac tromethamine loaded albumin microspheres for intramuscular administration. Curr Drug Deliv. 2013 Apr;10(2):158-66. PubMed PMID: 23157434. 15: Schoenberger SD, Kim SJ, Sheng J, Calcutt MW. Reduction of vitreous prostaglandin E2 levels after topical administration of ketorolac 0.45%. JAMA Ophthalmol. 2014 Feb;132(2):150-4. doi: 10.1001/jamaophthalmol.2013.5692. PubMed PMID: 24264034. 16: Bacon R, Newman S, Rankin L, Pitcairn G, Whiting R. Pulmonary and nasal deposition of ketorolac tromethamine solution (SPRIX) following intranasal administration. Int J Pharm. 2012 Jul 15;431(1-2):39-44. doi: 10.1016/j.ijpharm.2012.04.023. Epub 2012 Apr 13. PubMed PMID: 22525081. 17: Ramakrishnan S, Baskaran P, Talwar B, Venkatesh R. Prospective, Randomized Study Comparing the Effect of 0.1% Nepafenac and 0.4% Ketorolac Tromethamine on Macular Thickness in Cataract Surgery Patients With Low Risk for Cystoid Macular Edema. Asia Pac J Ophthalmol (Phila). 2015 Jul-Aug;4(4):216-20. doi: 10.1097/APO.0000000000000089. PubMed PMID: 26225780. 18: Drover DR, Hammer GB, Anderson BJ. The pharmacokinetics of ketorolac after single postoperative intranasal administration in adolescent patients. Anesth Analg. 2012 Jun;114(6):1270-6. doi: 10.1213/ANE.0b013e31824f92c2. Epub 2012 Mar 30. PubMed PMID: 22467894. 19: Guo Y, Kenney SR, Cook L, Adams SF, Rutledge T, Romero E, Oprea TI, Sklar LA, Bedrick E, Wiggins CL, Kang H, Lomo L, Muller CY, Wandinger-Ness A, Hudson LG. A Novel Pharmacologic Activity of Ketorolac for Therapeutic Benefit in Ovarian Cancer Patients. Clin Cancer Res. 2015 Nov 15;21(22):5064-72. doi: 10.1158/1078-0432.CCR-15-0461. Epub 2015 Jun 12. PubMed PMID: 26071482; PubMed Central PMCID: PMC4644688. 20: Shafiee A, Bowman LM, Hou E, Hosseini K. Aqueous humor penetration of ketorolac formulated in DuraSite or DuraSite 2 delivery systems compared to Acular LS in rabbits. J Ocul Pharmacol Ther. 2013 Nov;29(9):812-6. doi: 10.1089/jop.2013.0016. Epub 2013 Aug 31. PubMed PMID: 23992042.