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MedKoo Cat#: 524944 | Name: Dazoxiben HCl
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Description:

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

Dazoxiben is an antithrombotic agent is a drug that reduces the formation of blood clots.

Chemical Structure

Dazoxiben HCl
Dazoxiben HCl
CAS#74226-22-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 524944

Name: Dazoxiben HCl

CAS#: 74226-22-5 (HCl)

Chemical Formula: C12H13ClN2O3

Exact Mass: 232.0848

Molecular Weight: 268.70

Elemental Analysis: C, 53.64; H, 4.88; Cl, 13.19; N, 10.43; O, 17.86

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,750.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Related CAS #
74226-22-5 (HCl) 78218-09-4 (free base)
Synonym
Dazoxiben hydrochloride; Dazoxiben HCl; UK-37248; UK37248; UK 37248; UK-37248-01; UK 37248-01; UK37248-01
IUPAC/Chemical Name
4-(2-(1H-Imidazol-1-yl)ethoxy)benzoic acid hydrochloride
InChi Key
PVKDFUXBDJPRGU-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H12N2O3.ClH/c15-12(16)10-1-3-11(4-2-10)17-8-7-14-6-5-13-9-14;/h1-6,9H,7-8H2,(H,15,16);1H
SMILES Code
O=C(O)C1=CC=C(OCCN2C=CN=C2)C=C1.[H]Cl
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Dazoxiben is an antithrombotic agent.
In vitro activity:
The effect of the thromboxane synthetase inhibitor dazoxiben (UK 37248) on 113Indium-labelled platelet deposition on Dacron arterial grafts was examined in an artificial circulation containing human blood which mimics the haemodynamics of femoropopliteal bypass. The influence of this drug on thromboxane production and platelet reactivity was measured during the experiment. In vitro dazoxiben reduced plasma thromboxane by about 80%. After graft perfusion the mean (± s.e.mean) plasma thromboxane level in the active circuits at 354.3 ±46.3 pg/ml was significantly lower than that in the control circuits of 2013±301 pg/ml (P<0.05) with both post-perfusion circuits having elevated levels compared with the mean pre-circuit value of 79.1±28.7pg/ml (Figure 1). Reference: Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):61S-65S. https://pubmed.ncbi.nlm.nih.gov/6681706/
In vivo activity:
The effects of pretreatment with the thromboxane synthetase inhibitor UK 37248 (dazoxiben) administered 30 min before intravenous endotoxin (S. enteriditis) in the rat was investigated. UK 37248 pretreatment resulted in a significant (P less than 0.001) decrease in plasma iTXB2 at 30 min and 4 h to 193 +/- 28 pg/ml (n = 5) and 421 +/- 57 pg/ml (n = 5), respectively. Unexpectedly UK 37248 also significantly decreased plasma i6-keto PGF1 alpha at 30 min and 4 h to 360 +/- 75 pg/ml (n = 10) (P less than 0.005) and 1920 +/- 513 pg/ml (n = 10) (P less than 0.05), respectively. UK 37248 significantly (P less than 0.05) reduced the endotoxin mortality rate at 24 h from 69% (n = 13) to 30% (n = 13), UK 37248 also reduced splanchnic infarction from 90% (n = 20) to 6% (n = 16). UK 37248 significantly improved the endotoxin-induced thrombocytopaenia, disseminated intravascular coagulation, hypoglycaemia and lysosomal labilization. Reference: Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):133S-139S. https://pubmed.ncbi.nlm.nih.gov/6337604/
Solvent mg/mL mM
Solubility
DMSO 58.0 215.86
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 268.70 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. Halushka PV, Cook JA, Wise WC. Beneficial effects of UK 37248, a thromboxane synthetase inhibitor, in experimental endotoxic shock in the rat. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):133S-139S. doi: 10.1111/j.1365-2125.1983.tb02124.x. PMID: 6337604; PMCID: PMC1427698. 2. Hanson SR, Harker LA. Effect of dazoxiben on arterial graft thrombosis in the baboon. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):57S-60S. doi: 10.1111/j.1365-2125.1983.tb02108.x. PMID: 6681705; PMCID: PMC1427679. 3. Goldman M, Hall C, Hawker RJ, McCollum CN. Dazoxiben examined for platelet inhibitory effect in an artificial circulation. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):61S-65S. doi: 10.1111/j.1365-2125.1983.tb02109.x. PMID: 6681706; PMCID: PMC1427697.
In vitro protocol:
1. Goldman M, Hall C, Hawker RJ, McCollum CN. Dazoxiben examined for platelet inhibitory effect in an artificial circulation. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):61S-65S. doi: 10.1111/j.1365-2125.1983.tb02109.x. PMID: 6681706; PMCID: PMC1427697.
In vivo protocol:
1. Halushka PV, Cook JA, Wise WC. Beneficial effects of UK 37248, a thromboxane synthetase inhibitor, in experimental endotoxic shock in the rat. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):133S-139S. doi: 10.1111/j.1365-2125.1983.tb02124.x. PMID: 6337604; PMCID: PMC1427698. 2. Hanson SR, Harker LA. Effect of dazoxiben on arterial graft thrombosis in the baboon. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):57S-60S. doi: 10.1111/j.1365-2125.1983.tb02108.x. PMID: 6681705; PMCID: PMC1427679.
1: Dazoxiben. Lancet. 1983 Mar 19;1(8325):627-8. PMID: 6131306. 2: Hendra T, Collins P, Penny W, Sheridan D. Dazoxiben in stable angina. Lancet. 1983 May 7;1(8332):1041. doi: 10.1016/s0140-6736(83)92661-2. PMID: 6133076. 3: Jones EW, Cockbill SR, Cowley AJ, Hanley SP, Heptinstall S. Effects of dazoxiben and low-dose aspirin on platelet behaviour in man. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):39S-44S. doi: 10.1111/j.1365-2125.1983.tb02105.x. PMID: 6401999; PMCID: PMC1427688. 4: Reines HD, Halushka PV, Olanoff LS, Hunt PS. Dazoxiben in human sepsis and adult respiratory distress syndrome. Clin Pharmacol Ther. 1985 Apr;37(4):391-5. doi: 10.1038/clpt.1985.60. PMID: 3979000. 5: Butendieck RR, Murray PM. Raynaud disease. J Hand Surg Am. 2014 Jan;39(1):121-4. doi: 10.1016/j.jhsa.2013.08.117. Epub 2013 Nov 6. PMID: 24211176. 6: Sills T, Cowley AJ, Heptinstall S. Aspirin and dazoxiben as inhibitors of platelet behaviour: modification of their effects by agents that alter cAMP production. Thromb Res. 1986 Apr 1;42(1):91-8. doi: 10.1016/0049-3848(86)90200-8. PMID: 3010495. 7: Su KY, Sharma M, Kim HJ, Kaganov E, Hughes I, Abdeen MH, Ng JHK. Vasodilators for primary Raynaud's phenomenon. Cochrane Database Syst Rev. 2021 May 17;5(5):CD006687. doi: 10.1002/14651858.CD006687.pub4. PMID: 33998674; PMCID: PMC8127538. 8: Belch JJ, Cormie J, Newman P, McLaren M, Barbenel J, Capell H, Leiberman P, Forbes CD, Prentice CR. Dazoxiben, a thromboxane synthetase inhibitor, in the treatment of Raynaud's syndrome: a double-blind trial. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):113S-116S. doi: 10.1111/j.1365-2125.1983.tb02119.x. PMID: 6337601; PMCID: PMC1427695. 9: Irisarri E, Kessedjian MJ, Charuel C, Faccini JM, Greaves P, Monro AM, Nachbaur J, Rabémampianina Y. Dazoxiben, a prototype inhibitor of thromboxane synthesis, has little toxicity in laboratory animals. Hum Toxicol. 1985 May;4(3):311-5. doi: 10.1177/096032718500400312. PMID: 4040117. 10: Randall MJ. Selective inhibition of thromboxane synthesis with dazoxiben in animals and man. Thromb Res Suppl. 1983;4:81-5. doi: 10.1016/0049-3848(83)90362-6. PMID: 6415861. 11: Burke SE, Lefer AM, Smith GM, Smith JB. Prevention of extension of ischaemic damage following acute myocardial ischaemia by dazoxiben, a new thromboxane synthetase inhibitor. Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):97S-101S. doi: 10.1111/j.1365-2125.1983.tb02116.x. PMID: 6681711; PMCID: PMC1427699. 12: Ettinger WH, Wise RA, Schaffhauser D, Wigley FM. Controlled double-blind trial of dazoxiben and nifedipine in the treatment of Raynaud's phenomenon. Am J Med. 1984 Sep;77(3):451-6. doi: 10.1016/0002-9343(84)90101-3. PMID: 6540986. 13: Rui YC, Sun DX, Lin AY. [Effect of dazoxiben on the metabolism of arachidonic acid in isolated porcine basilar arteries]. Zhongguo Yao Li Xue Bao. 1990 May;11(3):261-4. Chinese. PMID: 2128432. 14: Patrignani P, Filabozzi P, Catella F, Pugliese F, Patrono C. Differential effects of dazoxiben, a selective thromboxane-synthase inhibitor, on platelet and renal prostaglandin-endoperoxide metabolism. J Pharmacol Exp Ther. 1984 Feb;228(2):472-7. PMID: 6537977. 15: Luderer JR, Nicholas GG, Neumyer MM, Riley DL, Vary JE, Garcia G, Schneck DW. Dazoxiben, a thromboxane synthetase inhibitor, in Raynaud's phenomenon. Clin Pharmacol Ther. 1984 Jul;36(1):105-15. doi: 10.1038/clpt.1984.147. PMID: 6428793. 16: Tindall H, Tooke JE, Menys VC, Martin MF, Davies JA. Effect of dazoxiben, a thromboxane synthetase inhibitor on skin-blood flow following cold challenge in patients with Raynaud's phenomenon. Eur J Clin Invest. 1985 Feb;15(1):20-3. doi: 10.1111/j.1365-2362.1985.tb00138.x. PMID: 3921380. 17: Sathler PC, Santana M, Lourenço AL, Rodrigues CR, Abreu P, Cabral LM, Castro HC. Human thromboxane synthase: comparative modeling and docking evaluation with the competitive inhibitors Dazoxiben and Ozagrel. J Enzyme Inhib Med Chem. 2014 Aug;29(4):527-31. doi: 10.3109/14756366.2013.817403. Epub 2013 Aug 5. PMID: 23914925. 18: Cowley AJ, Jones EW, Carter AJ, Hanley SP, Heptinstall S. The effects of dazoxiben, an inhibitor of thromboxane synthetase, on cold-induced forearm vasoconstriction and platelet behaviour in different individuals. Br J Clin Pharmacol. 1985 Jan;19(1):1-8. doi: 10.1111/j.1365-2125.1985.tb02605.x. PMID: 2983748; PMCID: PMC1463776. 19: Horgan MJ, Fenton JW 2nd, Malik AB. Alpha-thrombin-induced pulmonary vasoconstriction. J Appl Physiol (1985). 1987 Nov;63(5):1993-2000. doi: 10.1152/jappl.1987.63.5.1993. PMID: 3693233. 20: van Ooijen B, Ouwendijk RJ, Kort WJ, Zijlstra FJ, Vincent JE, Wilson JH, Westbroek DL. Raised plasma thromboxane B2 levels in experimental acute necrotizing pancreatitis in rats. The effects of flunarizine, dazoxiben, and indomethacin. Scand J Gastroenterol. 1988 Mar;23(2):188-92. doi: 10.3109/00365528809103966. PMID: 3363291.