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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-MPAM-15
MPAM-15

Chemical Structure : MPAM-15

CAS No.: 311783-51-4

MPAM-15 (MPAM15)

货号: PC-26060Not For Human Use, Lab Use Only.

MPAM-15 is a potent, selective, brain penetrant positive allosteric modulator of μ-opioid (MOR) receptor with pEC50 of 9.9, >16-fold selectivity for μOR over δOR, κOR, and NOPR.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MPAM-15 is a potent, selective, brain penetrant positive allosteric modulator of μ-opioid (MOR) receptor with pEC50 of 9.9, >16-fold selectivity for μOR over δOR, κOR, and NOPR.
MPAM-15 demonstrates 33- and threefold higher PAM cooperativity for DAMGO-induced μOR activation compared to BMS122 and BMS187, respectively.
MPAM-15 also exhibits comparable PAM activity at δOR and κOR.
MPAM-15 allosterically stabilizes the active conformation of μOR.
MPAM-15 enhances morphine-induced antinociception without increasing side effects.
The combination of MPAM-15 (15 or 30 mg/kg) with morphine (5 mg/kg) achieved analgesia equivalent to that of morphine (10 mg/kg) but without inducing comparable respiratory depression or constipation.

物理化学性质&存储条件

分子量 450.96
分子式 C27H27ClO4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

9-(5-(4-chlorophenyl)furan-2-yl)-3,3,6,6-tetramethyl-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione

参考文献

1. Wang Y, et al. Sci Adv. 2026 Feb 13;12(7):eaea9832.

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