2. GPCR/G Protein
  3. Endothelin Receptor
  4. J-104132

J-104132 (L-753037) 是一种强效、口服活性的、选择性和竞争性的 ETA/ETB 受体 (ETA/ETB receptor) 拮抗剂，其对 ETA 和 ETB 受体的 Ki 值分别为 0.034 nM 和 0.104 nM。J-104132 在体外可抑制 ET-1 (HY-P71446) 诱导的信号传导和血管收缩。J-104132 通过双重阻断 ETA/ETB 受体，在体内可减轻高血压、血管重塑和糖尿病内皮功能障碍。J-104132 可用于糖尿病血管并发症的研究[1][3]。

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J-104132

J-104132 Chemical Structure

CAS No. : 198279-45-7

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J-104132 相关抗体

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ETA ETB

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications[1][3].

IC50 & Target[1]

ETA

0.034 nM (Ki)

ETB

0.104 nM (Ki)

体外研究
(In Vitro)

J-104132 能有效抑制 ET-1 刺激的人 ETA/CHO 细胞中磷脂酰肌醇水解 (IC50 = 0.059 nM)，但在完全抑制浓度 (3 nM) 下自身不引发任何反应[1]。
J-104132 (0.001-10 μM) 可特异性竞争性拮抗 ET-1 诱导的兔髂动脉收缩，使 ET-1 浓度-反应曲线右移但不影响最大反应，且不抑制 KCl 或 Norepinephrine (HY-13715) 诱导的收缩[1]。
J-104132 (3 nM，20 分钟) 不改变糖尿病大鼠主动脉中 Ach (HY-B0282) 诱导的舒张作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

J-104132 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Note AUC CLplasma MRT Vd Cmax Tmax F
Rat[1] 0.3 mg/kg i.v. AUC0-10h 246 ng·h/mL 21.3 mL/min/kg 1.12 h 1.27 L/kg / / /
Rat[1] 1 mg/kg i.v. AUC0-10h 936 ng·h/mL 17.9 mL/min/kg 0.89 h 0.97 L/kg / / /
Rat[1] 1 mg/kg p.o. AUC0-10h 408 ng·h/mL / 3.10 h / 178.0 ng/mL 0.25 h 44 %
Rat[1] 10 mg/kg p.o. AUC0-10h 4028 ng·h/mL / 2.82 h / 1754.3 ng/mL 0.75 h /
Rat[1] 3 mg/kg i.v. AUC0-10h 3686 ng·h/mL 16.7 mL/min/kg 0.76 h 0.72 L/kg / / /
Rat[1] 3 mg/kg p.o. AUC0-10h 1252 ng·h/mL / 2.89 h / 476.8 ng/mL 0.40 h 34 %
体内研究
(In Vivo)

J-104132 (1、3 和 10 mg/kg，单次口服) 可剂量依赖性地且持续地抑制 SD 大鼠由 Big ET-1 诱导的升压反应[1]。
J-104132 (0.1、0.3 和 1 mg/kg，单次口服或静脉注射) 可剂量依赖性地抑制 SD 大鼠由 ET-1 诱导的升压反应[1]。
J-104132 (0.01、0.03、0.1 和 0.3 mg/kg/h，静脉输注 2 小时) 可剂量相关性地使犬的 ET-1 剂量反应曲线右移[1]。
J-104132 (10 mg/kg，灌胃给药，于球囊损伤后 12 小时开始，持续 2 周) 可降低雄性 SD 大鼠以及雄性和雌性 ETB 缺陷型大鼠的新生内膜/中膜比值，但对雌性野生型大鼠无效[2]。
J-104132 (10 mg/kg，口服，每日一次，于 STZ 注射 7 周后开始给药，持续 4 周) 能够恢复 Streptozotocin (STZ) (HY-13753) 诱导的糖尿病大鼠中受损的乙酰胆碱 (ACh) 介导的内皮依赖性血管舒张功能[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rats (6-7 weeks) challenged with big ET-1 (0.5 nmol/kg, i.v.)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: p.o., single dose
Result: Almost completely inhibited the pressor response elicited by big ET-1 at 30 min after administration at doses of 1, 3, and 10 mg/kg.
Gradually recovered inhibition of the pressor response elicited by big ET-1 within 3 to 4 h at 1 mg/kg.
Inhibition was maintained for more than 8 hours after administration of the 3 and 10 mg/kg doses.
Animal Model: Male SD rats (200-400 g) challenged with ET-1 (0.5 nmol/kg, i.v.)[1]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: p.o. or i.v., single dose
Result: Showed dose-related inhibition of ET-1-induced pressor responses after p.o. and i.v. administration.
The relative potencies of J-104132 after p.o. administration were three times less than those after i.v. administration.
Animal Model: Mongtrl dogs (10-15 kg) challenged with ET-1 (1-100 pmol/min for 30 min into the renal artery)[1]
Dosage: 0.01, 0.03, 0.1 and 0.3 mg/kg/h
Administration: i.v., infusion for 2 h
Result: Shifted ET-1 dose-response curve to the right in a dose-related manner.
Shifted the ET-1 dose-response curve approximately 12-fold at 0.03 mg/kg/h.
Animal Model: Mongtrl dogs (10-15 kg) challenged with ET-1 (1-100 pmol/min for 30 min into the brachial artery)[1]
Dosage: 0.01, 0.03, 0.1 and 0.3 mg/kg/h
Administration: i.v., infusion for 2 h
Result: Led to a 15- to 20-fold shift in the dose-response curve at 0.3 mg/kg/h compared with the vehicle.
Shifted the dose-response curve to ET-1 in this vascular bed by more than 20-fold at dose of 0.3 mg/kg/h.
Showed no marked alterations in heart rate, although systemic arterial pressure was observed to slowly decline by approximately 18% over the entire protocol period at the 0.3 mg/kg/h dosage.
Animal Model: Male and female Wild-type and ETB-deficient rats (12-15 weeks) challenged with balloon injury procedure[2]
Dosage: 10 mg/kg
Administration: i.g., for 2 weeks starting 12 h after balloon injury
Result: Markedly decreased the neointima/media ratio in both the wild-type and ETB-deficient male rats.
Markedly decreased the neointima/media ratio in the ETB-deficient female rats but not in the wild-type female rats.
The ETB-deficient rats exhibited significantly increased plasma ET-1 levels, in both males and females compared with the wild-type rats.
Showed no significant differences in ETA or ETB receptor mRNA expression.
Animal Model: Male and female SD rats (10 weeks) challenged with balloon injury procedure[2]
Dosage: 10 mg/kg
Administration: i.g., for 2 weeks starting 12 h after balloon injury
Result: Did not affect body weight, uteri wet weight, or SBP for 2 weeks treatment.
Significantly decreased the neointima/media ratio in the male rats.
Did not affect the neointima/media ratio in female rats.
Significantly increased plasma ET-1 levels compared with vehicle treated group in female SD rats.
Animal Model: Male Wistar rats (7 weeks) injected with STZ (75 mg/kg)[3]
Dosage: 10 mg/kg
Administration: p.o., daily for 4 weeks starting 7 weeks after STZ
Result: Significantly attenuated the impairment of ACh-induced endothelium-dependent relaxation in diabetic rats.
Did not alter plasma glucose, total cholesterol, HDL, VLDL, LDL or triglyceride in diabetic rats.
Revealed that the expression ratio eNOS/GAPDH did not differ among groups.
Reversed the increase of the expression of p22phox mRNA induced by diabetic in rats.
Significantly decreased the elevated level of superoxide anion in the aortae of diabetic rats.
分子量

531.60

Formula

C31H33NO7
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

J-104132 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

J-104132198279-45-7J104132J 104132Endothelin ReceptorETA/ETB receptorET-1vascular contractionshypertensiondiabetic vascular complicationsdiabeticInhibitorinhibitorinhibit

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