157284-96-3

157284-96-3 structure

Name: Antalarmin
Chemical Name: N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number: 157284-96-3
Molecular Formula: C₂₄H₃₄N₄
Molecular Weight: 378.55400
Catalog: Signaling Pathways GPCR/G Protein CRFR
Create Date: 2016-02-27 04:07:57
Modify Date: 2025-08-26 11:37:18
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].

Name	N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
Synonyms	7H-Pyrrolo(2,3-d)pyrimidin-4-amine,N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl) Antalarmin

Description	Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> CRFR Research Areas >> Neurological Disease
Target	Ki: 2.7 nM (CRHR1)[3]
In Vitro	Antalarmin 通过 cAMP/PKA 信号通路抑制促肾上腺皮质激素释放因子 (CRF) 对 Aβ1-42 水平的影响[2]。 Western Blot Analysis[2] Cell Line: Primary hippocampal neurons derived from Tg2576 mice Concentration: 100 nM Incubation Time: 48 h Result: Blocked CRF-induced increases in PKAIIβ levels.
In Vivo	Antalarmin (10 mg/kg; i.p.; daily for 4 weeks) 可以改善小鼠的慢性轻度应激 (CMS) 诱导的变化[1]。 Antalarmin (20 mg/kg; i.p.; daily for 7 days) 显著降低亚急性应激 Tg2576 小鼠中 Aβ1-42 水平[2]。 Animal Model: BALB/cByJIco male mice, chronic mild stress model[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection, daily for 4 weeks Result: Induced a significant improvement of mice physical state. Induced a nonsignificant decrease of the lit box (TLB) and activity when compared to controls.
References	[1]. Ducottet C, et al. Effects of the selective nonpeptide corticotropin-releasing factor receptor 1 antagonist antalarmin in the chronic mild stress model of depression in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Jun;27(4):625-31. [2]. Dong H, et al. Effects of corticotrophin-releasing factor receptor 1 antagonists on amyloid-β and behavior in Tg2576 mice. Psychopharmacology (Berl). 2014 Dec;231(24):4711-22. [3]. Zorrilla EP, et al. Urocortin shares the memory modulating effects of corticotropin-releasing factor (CRF): mediation by CRF1 receptors. Brain Res. 2002 Oct 18;952(2):200-10.

Density	1.05g/cm3
Boiling Point	437.2ºC at 760mmHg
Molecular Formula	C₂₄H₃₄N₄
Molecular Weight	378.55400
Flash Point	218.2ºC
Exact Mass	378.27800
PSA	33.95000
LogP	5.89730
Vapour Pressure	7.63E-08mmHg at 25°C
Index of Refraction	1.574

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.

157284-96-3	220953-69-5
89352-67-0	76653-80-0
1207279-23-9	2320820-61-7
2310082-03-0	2309541-06-6
2140787-15-9	2320821-04-1
2142247-90-1	2320142-41-2
2310013-84-2