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首页-小分子抑制剂&激动剂-GPCR-Mas-related G protein-coupled receptor (MRGPR)-BCFTP
BCFTP

Chemical Structure : BCFTP

CAS No.: 2781215-95-8

BCFTP

货号: PC-25931Not For Human Use, Lab Use Only.

BCFTP is a specific, orally bioavailable positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1), BCFTP selectively potentiates the functional response of MrgprX1 in HEK293 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BCFTP is a specific, orally bioavailable positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1), BCFTP selectively potentiates the functional response of MrgprX1 in HEK293 cells.
Oral administration of BCFTP dose-dependently inhibited heat hyperalgesia and spontaneous pain-like behavior but not mechanical hypersensitivity after sciatic chronic constrictive injury (CCI) in MrgprX1 mice.
BCFTP enhanced BAM8-22–induced, MrgprX1-mediated reduction of C-fiber eEPSC amplitudes in spinal lamina II neurons, indicating inhibition of spinal nociceptive synaptic transmission.
BCFTP ameliorated certain pain-related behaviors in transgenic mice expressing the human receptor but did not induce itch, a common side effect of agonists for this receptor family.

物理化学性质&存储条件

分子量 496.90
分子式 C23H17ClF4N2O2S
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

6-tert-butyl-5-(4-chlorophenyl)-4-(2-fluoro-6-(trifluoromethoxy)phenoxy)thieno[2,3-d]pyrimidine

参考文献

1. Uniyal A, et al. Sci Transl Med. 2025 Dec 17;17(829):eadw9446.

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