Rocepafant | BN-50730 | CAS#132579-32-9 | PAF antagonist

MedKoo Cat#: 326906 | Name: Rocepafant

Description:

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

Rocepafant, also known as BN-50730; LAU-8080, is a platelet activating factor (PAF) antagonist potentially for the treatment of asthma. BN 50730 attenuates hypoxic-ischemic brain injury in neonatal rats. BN 50730 also showed activity to inhibit tumor necrosis factor-alfa-mediated cytotoxicity on murine L929 tumor cells.

Chemical Structure

Rocepafant

CAS#132579-32-9

Theoretical Analysis

MedKoo Cat#: 326906

Name: Rocepafant

CAS#: 132579-32-9

Chemical Formula: C26H23ClN6OS2

Exact Mass: 534.1063

Molecular Weight: 535.08

Elemental Analysis: C, 58.36; H, 4.33; Cl, 6.63; N, 15.71; O, 2.99; S, 11.98

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.

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Related CAS #

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Synonym

BN-50730; BN 50730; BN50730; LAU-8080; LAU 8080; LAU8080; Rocepafant

IUPAC/Chemical Name

6-(2-chlorophenyl)-N-(4-methoxyphenyl)-1-methyl-7,10-dihydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-9(8H)-carbothioamide

InChi Key

WBGAFGNZNGJVNW-UHFFFAOYSA-N

InChi Code

InChI=1S/C26H23ClN6OS2/c1-15-30-31-22-13-28-24(18-5-3-4-6-20(18)27)23-19-11-12-32(14-21(19)36-25(23)33(15)22)26(35)29-16-7-9-17(34-2)10-8-16/h3-10H,11-14H2,1-2H3,(H,29,35)

SMILES Code

CC1=NN=C2N1C3=C(C4=C(CN(C(NC5=CC=C(OC)C=C5)=S)CC4)S3)C(C6=CC=CC=C6Cl)=NC2

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 535.08 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

1: Liu XH, Eun BL, Barks JD. Platelet-activating factor antagonist BN 50730 attenuates hypoxic-ischemic brain injury in neonatal rats. Pediatr Res. 2001 Jun;49(6):804-11. PubMed PMID: 11385142. 2: Singh N, Sharma A, Singh M. Effects of BN-50730 (PAF receptor antagonist) and physostigmine (AChE inhibitor) on learning and memory in mice. Methods Find Exp Clin Pharmacol. 1997 Nov;19(9):585-8. PubMed PMID: 9500121. 3: Silva CL, Cruz HN, Violante FA, Cordeiro RS, Martins MA, Noël F. Formation of a highly stable complex between BN 50730 [tetrahydro-4,7,8,10 methyl-1(chloro-2 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4',3'-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-a] diazepine-1,4] and the platelet-activating factor receptor in rabbit platelet membranes. Biochem Pharmacol. 1996 Jan 26;51(2):193-6. PubMed PMID: 8615889. 4: Hilliquin P, Guinot P, Chermat-Izard V, Puechal X, Menkes CJ. Treatment of rheumatoid arthritis with platelet activating factor antagonist BN 50730. J Rheumatol. 1995 Sep;22(9):1651-4. PubMed PMID: 8523338. 5: Cakici I, Mataraci N, Ersoy S, Tunçtan B, Abacioğlu N, Kanzik I. Effects of platelet-activating factor antagonists WEB 2086 and BN 50730 on digoxin-induced arrhythmias. Pharmacol Toxicol. 1995 Jun;76(6):343-7. PubMed PMID: 7479573. 6: Hilliquin P, Natour J, Aissa J, Guinot P, Laoussadi S, Benveniste J, Menkes CJ, Arnoux B. Treatment of carrageenan induced arthritis by the platelet activating factor antagonist BN 50730. Ann Rheum Dis. 1995 Feb;54(2):140-3. PubMed PMID: 7702404; PubMed Central PMCID: PMC1005539. 7: Pires AL, e Silva PM, Pasquale C, Castro-Faria-Neto HC, Bozza PT, Cordeiro RS, Rae GA, Braquet P, Lagente V, Martins MA. Long-lasting inhibitory activity of the hetrazepinic BN 50730 on exudation and cellular alterations evoked by PAF and LPS. Br J Pharmacol. 1994 Nov;113(3):994-1000. PubMed PMID: 7858896; PubMed Central PMCID: PMC1510468. 8: Lagente V, Boichot E, Carre C, Guinot P, Mencia-Huerta JM, Braquet P. Effects of the platelet activating factor antagonists BN 52021 and BN 50730 on antigen-induced bronchial hyperresponsiveness and eosinophil infiltration in lung from sensitized guinea-pigs. Clin Exp Allergy. 1993 Dec;23(12):1002-10. PubMed PMID: 10779293. 9: Hunyadi J, Kenderessy AS, Duda E, Braquet P, Dobozy A. Platelet-activating factor antagonists (BN 52021 and BN 50730) inhibit tumor necrosis factor-alfa-mediated cytotoxicity on murine L929 tumor cells. Mol Immunol. 1993 Apr;30(6):517-9. PubMed PMID: 7683748. 10: Doly M, Cluzel J, Millerin M, Bonhomme B, Braquet P. Prevention of chloroquine-induced electroretinographic damage by a new platelet-activating factor antagonist, BN 50730. Ophthalmic Res. 1993;25(5):314-8. PubMed PMID: 8259265. 11: Dyson MC, Bellan JA, Minkes RK, Beckerman RC, Wegmann MJ, Braquet P, McNamara DB, Kadowitz PJ. Influence of SK&F 95587 and BN 50730 on bronchoconstrictor responses in the cat. J Pharmacol Exp Ther. 1990 Dec;255(3):1320-7. PubMed PMID: 2175802.