WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H584249
CAS#: 141594-26-5
Description: BQ 484 is an endothelin ET (a) receptor antagonisht.
Hodoodo Cat#: H584249
Name: BQ 485
CAS#: 141594-26-5
Chemical Formula: C35H44N6O5
Exact Mass: 628.34
Molecular Weight: 628.774
Elemental Analysis: C, 66.86; H, 7.05; N, 13.37; O, 12.72
This product is not in stock, which may be available by custom synthesis.
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Synonym: BQ 485; BQ485; BQ-485
IUPAC/Chemical Name: N-(N-(N-((Hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl)-D-tryptophyl)-D-tryptophan
InChi Key: ZBJNAHVLKNFOPP-OJDZSJEKSA-N
InChi Code: InChI=1S/C35H44N6O5/c1-22(2)17-29(40-35(46)41-15-9-3-4-10-16-41)32(42)38-30(18-23-20-36-27-13-7-5-11-25(23)27)33(43)39-31(34(44)45)19-24-21-37-28-14-8-6-12-26(24)28/h5-8,11-14,20-22,29-31,36-37H,3-4,9-10,15-19H2,1-2H3,(H,38,42)(H,39,43)(H,40,46)(H,44,45)/t29-,30+,31+/m0/s1
SMILES Code: O=C(O)[C@@H](CC1=CNC2=C1C=CC=C2)NC([C@@H](CC3=CNC4=C3C=CC=C4)NC([C@H](CC(C)C)NC(N5CCCCCC5)=O)=O)=O
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 628.77 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Sakuma I, Asajima H, Fukao M, Tohse N, Tamura M, Kitabatake A. Effects of BQ-485, a selective ETA antagonist, on endothelin-mediated vasomotion in rat coronary vascular beds. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S400-3. PubMed PMID: 8587427.
2: Takasu A, Matsushima S, Takino M, Okada Y. Effect of an endothelin-1 antagonist, BQ-485, on cerebral oxygen metabolism after complete global cerebral ischemia in dogs. Resuscitation. 1997 Feb;34(1):65-9. PubMed PMID: 9051826.
3: Itoh S, Sasaki T, Ide K, Ishikawa K, Nishikibe M, Yano M. A novel endothelin ETA receptor antagonist, BQ-485, and its preventive effect on experimental cerebral vasospasm in dogs. Biochem Biophys Res Commun. 1993 Sep 15;195(2):969-75. PubMed PMID: 8373429.
4: Holló G, Kóthy P, Lakatos P, Vargha P. Endothelin-A receptor antagonist BQ-485 protects against intraocular pressure spike induced by laser trabeculoplasty in the rabbit. Ophthalmologica. 2002 Nov-Dec;216(6):459-62. PubMed PMID: 12566893.
5: Mutsaers SE, Marshall RP, Goldsack NR, Laurent GJ, McAnulty RJ. Effect of endothelin receptor antagonists (BQ-485, Ro 47-0203) on collagen deposition during the development of bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 1998 Apr-Jun;11(2-3):221-5. PubMed PMID: 9918760.
6: Ihara M, Yamanaka R, Ohwaki K, Ozaki S, Fukami T, Ishikawa K, Towers P, Yano M. [3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur J Pharmacol. 1995 Feb 14;274(1-3):1-6. PubMed PMID: 7768260.
7: Taniai H, Suematsu M, Suzuki T, Norimizu S, Hori R, Ishimura Y, Nimura Y. Endothelin B receptor-mediated protection against anoxia-reoxygenation injury in perfused rat liver: nitric oxide-dependent and -independent mechanisms. Hepatology. 2001 Apr;33(4):894-901. PubMed PMID: 11283854.
8: Nakamura T, Hisaka A, Sawasaki Y, Suzuki Y, Fukami T, Ishikawa K, Yano M, Sugiyama Y. Carrier-mediated active transport of BQ-123, a peptidic endothelin antagonist, into rat hepatocytes. J Pharmacol Exp Ther. 1996 Aug;278(2):564-72. PubMed PMID: 8768705.
9: Ruetten H, Thiemermann C. Effect of selective blockade of endothelin ETB receptors on the liver dysfunction and injury caused by endotoxaemia in the rat. Br J Pharmacol. 1996 Oct;119(3):479-86. PubMed PMID: 8894167; PubMed Central PMCID: PMC1915700.
10: Tanaka K, Higuchi H, Karasawa F, Sato T. Effects of selective and non-selective endothelin antagonists on ischemia-reperfusion damage in the isolated perfused murine liver. Res Commun Mol Pathol Pharmacol. 1999 Feb;103(2):129-38. PubMed PMID: 10461680.
11: Doi S, Smedira N, Murray PA. Pulmonary vasoregulation by endothelin in conscious dogs after left lung transplantation. J Appl Physiol (1985). 2000 Jan;88(1):210-8. PubMed PMID: 10642383.
12: Shen J, Nakanishi T, Gu H, Miyagawa-Tomita S, Wu GR, Momma K, Nakazawa M. The role of endothelin in oxygen-induced contraction of the ductus arteriosus in rabbit and rat fetuses. Heart Vessels. 2002 Jul;16(5):181-8. PubMed PMID: 12181591.
13: Mori S, Kaneko H, Mitsuma T, Hayakawa T, Yamaguchi C, Uruma M. Implications of gastric topical bioactive peptides in ammonia-induced acute gastric mucosal lesions in rats. Scand J Gastroenterol. 1998 Apr;33(4):386-93. PubMed PMID: 9605260.
14: Oktar BK, Gülpinar MA, Bozkurt A, Ghandour S, Cetinel S, Moini H, Yeğen BC, Bilsel S, Granger DN, Kurtel H. Endothelin receptor blockers reduce I/R-induced intestinal mucosal injury: role of blood flow. Am J Physiol Gastrointest Liver Physiol. 2002 Apr;282(4):G647-55. PubMed PMID: 11897624.
15: Favuzza J, Hechtman HB. Hemostasis in the absence of clotting factors. J Trauma. 2004 Jul;57(1 Suppl):S42-4. PubMed PMID: 15280751.
16: Montagnani M, Potenza MA, Rinaldi R, Mansi G, Nacci C, Serio M, Vulpis V, Pirrelli A, Mitolo-Chieppa D. Functional characterization of endothelin receptors in hypertensive resistance vessels. J Hypertens. 1999 Jan;17(1):45-52. PubMed PMID: 10100093.
17: Tanaka K, Karasawa F, Sato T. [Effects of endothelin antagonists on isolated perfused murine livers in the early phase of warm ischemia-reperfusion injury under propofol anesthesia]. Masui. 1999 Oct;48(10):1113-20. Japanese. PubMed PMID: 10554503.
18: Günal O, Yeğen C, Aktan AO, Yalin R, Yeğen BC. Gastric functions in portal hypertension. Role of endothelin. Dig Dis Sci. 1996 Mar;41(3):585-90. PubMed PMID: 8617140.
19: Kumagai H, Suzuki H, Ichikawa M, Nishizawa M, Oshima N, Saruta T. Interaction between endothelin and nitric oxide in sympathetic nerve modulation in hypertensive rats. Hypertens Res. 1997 Mar;20(1):35-42. PubMed PMID: 9101311.
20: Deniz M, Cetinel S, Kurtel H. Blood flow alterations in TNBS-induced colitis: role of endothelin receptors. Inflamm Res. 2004 Jul;53(7):329-36. Epub 2004 Jun 25. PubMed PMID: 15241569.
