AC-262536

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AC-262536 是一种选择性雄激素受体 (SAR) 调节剂，对雄激素受体表现出有效的激动剂活性。

AC-262536 is a selective androgen receptor (SAR) modulator and exhibits potent agonist activity at the androgen receptor. It has partial agonist activity with respect to testosterone and suppresses luteinizing hormone.(In Vitro):AC-262536 inhibits dihydroxytestosterone (DHT)-induced proliferation of LNCaP in a dose-dependent manner. The effects are significant with 100 nM, and reaches a plateau with 1 μM.(In Vivo):In male sprague-dawley rats, administration of AC-262536 (subcutaneous injection, once daily for 14 consecutive days) significantly decreased LH levels by about 40% at the 3 mg/kg dose. At the 10 and 30 mg/kg doses, the effects of AC-262536 were significantly stronger than Testosterone Propionate (TP) : 1.91±0.32 ng/mL and 1.53±0.34 ng/mL vs. 3.12±0.69 ng/mL, respectively.

AC-262536 dose-dependently inhibits dihydroxytestosterone (DHT)-induced proliferation of LNCaP. The effects are significant with 100 nM AC-262536 (%inhibition 47.2±12.2), and reaches a plateau with 1 μM treatment (%inhibition 50.7±7.6). Thus, AC-262536 can act as a functional antagonist in prostate cells.

AC-262536 (3, 10, 30 mg/kg) reverses the luteinizing hormone (LH) spike in castrated rats. Animal Model:Male Sprague-Dawley rats (200-225 g)Dosage:3, 10 and 30 mg/kg Administration:Administered subcutaneously; once daily for 14 consecutive days Result:Significantly decreased LH levels by about 40% at the 3 mg/kg dose.The ED50 was determined to be 2.8 mg/kg.At the 10 and 30 mg/kg doses, the effects of AC-262536 were significantly stronger than Testosterone Propionate (TP) : 1.91±0.32 ng/mL and 1.53±0.34 ng/mL vs. 3.12±0.69 ng/mL, respectively.

AC 262536 | AC262536

Endocrinology/Hormones

Androgen Receptor (AR)

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870888-46-3

278.355

C18H18N2O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (179.63 mM)

OC1C[C@@H]2CC[C@H](C1)N2c1ccc(C#N)c2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years