SML3652
TASP0277308
≥98% (HPLC)
동의어(들):
(R)-3,4-Dichloro-N-(1-(4-ethyl-5-(3-(4-methylpiperazin-1-yl)phenoxy)-4H-1,2,4-triazol-3-yl)ethyl)benzenesulfonamide, 3,4-Dichloro-N-[(1R)-1-[4-ethyl-5-[3-(4-methyl-1-piperazinyl)phenoxy]-4H-1,2,4-triazol-3-yl]ethyl]benzenesulfonamide, TASP 0277308, TASP-0277308
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모든 사진(2)
About This Item
추천 제품
Quality Level
분석
≥98% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
-10 to -25°C
생화학적/생리학적 작용
TASP0277308 is an orally active, highly S1P1 subtype-selective sphingosine-1-phosphate (S1P) receptor antagonist (IC50 = 2.7/4.2 nM against 0.1 nM S1P for binding mouse/human S1P1; IC50 >8.7 μM for S1P2-5). TASP0277308 effectively inhibits S1P1-mediated GTPγS membrane binding, cAMP response and chemotaxis (IC50 = 7.8, 3.5, 15 nM, respectively, agianst 10 nM S1P; hS1P1-expressing HEK293 or CHO) and demonstrates in vivo efficacy in various animal disease models, including collagen-induced arthritis and tumor angiogenesis in mice (10-100 mg/kg bid po), as well as neuropathic pain in rats (0.6-3 mg/kg via acute po or ip, acute 30 nmol or daily 10 nmol intrathecal injection).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Sphingosine-1-phosphate receptor 1 activation in astrocytes contributes to neuropathic pain
Proceedings of the National Academy of Sciences of the USA, 116(21), 10557-10562 (2019)
Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activities
Journal of immunology (Baltimore, Md. : 1950), 188(1), 206-215 (2012)
Targeting the S1P/S1PR1 axis mitigates cancer-induced bone pain and neuroinflammation
Pain, 158(9), 1733-1742 (2017)
Sphingosine 1-Phosphate Receptor Subtype 1 as a Therapeutic Target for Brain Trauma
Journal of Neurotrauma, 35(13), 1452-1466 (2018)
S1P1 Modulator-Induced G ?i Signaling and ?-Arrestin Recruitment Are Both Necessary to Induce Rapid and Efficient Reduction of Blood Lymphocyte Count In Vivo
Molecular Pharmacology, 93(2), 109-118 (2018)
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
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