Dazoxiben Free Base

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

MedKoo CAT#: 413493

CAS#: 78218-09-4 (free base)

Description: Dazoxiben Free Base is an orally active thromboxane synthase inhibitor. It has shown a significant clinical improvement in patients with Raynaud's syndrome.

Chemical Structure

img
Dazoxiben Free Base
CAS# 78218-09-4 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 413493
Name: Dazoxiben Free Base
CAS#: 78218-09-4 (free base)
Chemical Formula: C12H12N2O3
Exact Mass: 232.08
Molecular Weight: 232.240
Elemental Analysis: C, 62.06; H, 5.21; N, 12.06; O, 20.67

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 74226-22-5 (HCl)   78218-09-4 (free base)    

Synonym: Dazoxiben Free Base; UK37248; UK-37248; UK 37248

IUPAC/Chemical Name: Benzoic acid, 4-(2-(1H-imidazol-1-yl)ethoxy)-

InChi Key: XQGZSYKGWHUSDH-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H12N2O3/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)

SMILES Code: O=C(O)C1=CC=C(OCCN2C=CN=C2)C=C1

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: 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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Dazoxiben is an antithrombotic agent is a drug that reduces the formation of blood clots.
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
To be determined 0.0 0.00

Preparing Stock Solutions

The following data is based on the product molecular weight 232.24 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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Dazoxiben. Lancet. 1983 Mar 19;1(8325):627-8. PMID: 6131306.

2: 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.

3: 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.

4: 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.

5: 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.

6: 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.

7: 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.

8: Rui YC, Sun DX, Long K. [Effect of dazoxiben on cerebrovascular resistance in rabbits]. Zhongguo Yao Li Xue Bao. 1989 Jul;10(4):342-5. Chinese. PMID: 2624120.