5.33797

C5aR Antagonist, DF2593A

• 동의어(들): C5aR Antagonist, DF2593A, (R)-4-(1-(4-(piperidin-1-yl)butanamido)ethyl)phenyl trifluoromethanesulfonate, C5aR Inhibitor, DF2593A, C5aR Blocker, DF2593A, C5a Receptor Antagonist, DF2593A
• 실험식(Hill 표기법): C₁₈H₂₅F₃N₂O₄S
• CAS Number: 938452-57-4
• Molecular Weight: 422.46
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 50 mg/mL
• 저장 온도: −20°C

설명

일반 설명

An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC₅₀ = 5.0 nM) and is also effective in rat and mouse orthologs (IC₅₀ = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (C_max = 100 nM; T_max = 1.2 h at 1 mg/kg in mice).

An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC₅₀ = 5.0 nM) and is also effective in rat and mouse orthologs (IC₅₀ = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (C_max = 100 nM; T_max = 1.2 h at 1 mg/kg in mice).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
C5aR

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Moriconi, A., et al. 2014. PNAS.111, 16937.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable