ChemicalBook > CAS DataBase List > A192621

A192621

Product Name
A192621
CAS No.
195529-54-5
Chemical Name
A192621
Synonyms
A192621;A192621,CID 5310991;A192621 >=98 (HPLC);(2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID;3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)-
CBNumber
CB23369698
Molecular Formula
C33H38N2O6
Formula Weight
558.66
MOL File
195529-54-5.mol
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A192621 Property

Boiling point:
738.3±60.0 °C(Predicted)
Density 
1.233±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: 2mg/mL, clear
form 
powder
pka
3.52±0.60(Predicted)
color 
white to beige
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2277
Product name
A192621
Purity
≥98 (HPLC)
Packaging
5mg
Price
$141.55
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2277
Product name
A192621
Purity
≥98 (HPLC)
Packaging
25mg
Price
$419.3
Updated
2025/07/31
ChemScene
Product number
CS-0077507
Product name
A-192621
Purity
≥99.0%
Packaging
5mg
Price
$380
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
BIO0000292
Product name
A-192621
Purity
95.00%
Packaging
5MG
Price
$504.64
Updated
2021/12/16
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A192621 Chemical Properties,Usage,Production

Uses

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].

Biological Activity

A192621 is a selective; orally available ETB endothelin receptor antagonist. A192621 has been shown to cause an increase in arterial blood pressure and to promote apoptosis in human pulmonary arterial smooth muscle cells.

in vivo

A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat[3].

Animal Model:Male Sprague-Dawley rats (250-350 g)[3]
Dosage:30 mg/kg 100 mg/kg
Administration:Oral administration; daily; for 3 days
Result:Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.

IC 50

ETB: 4.5 nM (IC50); ETB: 8.8 nM (Ki); ETA: 4280 nM (IC50); ETA: 5600 nM (Ki)

References

[1] Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. DOI:10.1042/CS103S107S
[2] Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120. DOI:10.1016/j.lfs.2016.03.044
[3] Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. DOI:10.1042/CS103S112S

A192621 Preparation Products And Raw materials

Raw materials

Preparation Products

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A192621 Suppliers

China 14 United States 5 Global 19
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
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United States
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12952
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Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
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58
Jinan Yaoyan Pharmaceutical Co., Ltd.
Tel
Fax
-
Email
jnyaoyan@163.com
Country
China
ProdList
3069
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58
Nanjing Meihao Pharmaceutical Technology Co., Ltd.
Tel
meitaochem@126.com
Email
meitaochem@126.com
Country
China
ProdList
19103
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58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
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58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
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China
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11218
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Energy Chemical
Tel
021-58432009 400-005-6266
Fax
021-58436166
Email
marketing1@energy-chemical.com
Country
China
ProdList
44894
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Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 15801484223;
Email
psaitong@jm-bio.com
Country
China
ProdList
29757
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JinOu Biomedical (Nanjing) Co., Ltd.
Tel
13000000000
Fax
jinoupharma@163
Email
jinoupharma@163.com
Country
China
ProdList
11721
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58
Beijing Biocreative Technology Co., Ltd.
Tel
15522676233
Email
3007606172@qq.com
Country
China
ProdList
1248
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58

195529-54-5, A192621Related Search:


  • (2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID
  • A192621
  • A192621,CID 5310991
  • 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)-
  • A192621 >=98 (HPLC)
  • 195529-54-5