A-216546
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- CAS号:
- 212481-66-8
- 英文名:
- A-216546
- 英文别名:
- ABT-546;A-216546;ABT 546,ABT546;3-Pyrrolidinecarboxylic acid, 1-[2-(dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)-, (2S,3R,4S)-
- 中文名:
- A-216546
- 中文别名:
- 化合物 T10225
- CBNumber:
- CB48054298
- 分子式:
- C30H48N2O6
- 分子量:
- 532.71
- MOL File:
- 212481-66-8.mol
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A-216546化学性质
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沸点:
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636.9±55.0 °C(Predicted)
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密度:
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1.097±0.06 g/cm3(Predicted)
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酸度系数(pKa):
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3.58±0.60(Predicted)
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A-216546性质、用途与生产工艺
ABT-546 (A-216546) 是一种有效的，高选择性和活性的内皮素 ETA 受体拮抗剂，对 [125I]-内皮素-1 与克隆的人 ETA 结合的 Ki 为 0.46 nM。ABT-546 对 ETA 的选择性比对 ETB 受体的选择性高 25,000 倍以上。ABT-546 阻断内皮素-1 诱导的花生四烯酸释放和磷脂酰肌醇水解，IC50 分别为 0.59 nM 和 3 nM。
ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ET
A
receptor in membranes prepared from rat pituitary MMQ cells with an IC
50
value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [
125
I]endothelin-3 binding to endothelin ET
B
rceptor in membranes prepared from porcine cerebellum with an IC
50
value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ET
A
and ET
B
receptors, ABT-546 again effectively inhibits specific [
125
I]endothelin-1 binding to endothelin ET
A
receptor with an IC
50
value of 0.49 nM, but is less effective in inhibiting specific [
125
I]endothelin-3 binding to endothelin ET
B
receptor with an IC
50
value of 15,400 nM.
In isolated vessels, ABT-546 inhibits endothelin ET
A
receptor-mediated endothelin-1-induced vasoconstriction, and endothelin ET
B
receptor-mediated sarafotoxin 6c-induces vasoconstriction with pA
2
of 8.29 and 4.57, respectively.
ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats.
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Animal Model:
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Male Sprague-Dawley rats (250-350 g) induced with endothelin-1
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Dosage:
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0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:
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Oral administration; for 1 hour or 4 hours
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Result:
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Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
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A-216546
上下游产品信息
上游原料
下游产品
212481-66-8, A-216546 相关搜索:
- 化合物 T10225
- 212481-66-8
- 3-Pyrrolidinecarboxylic acid, 1-[2-(dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)-, (2S,3R,4S)-
- ABT 546,ABT546
- A-216546
- ABT-546