5.33683

PMX53

≥98% (HPLC), solid, C5aR antagonist, Calbiochem^®

• 別名: C5aR Antagonist, PMX53, Ac-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
• 実験式（ヒル表記法）: C₄₇H₆₅N₁₁O₇ · xC₂HF₃O₂
• CAS番号: 219639-75-5
• 分子量: 896.09 (free base basis)
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• product name: C5aR Antagonist, PMX53,
• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable, orally available, and metabolically stable macrocyclic hexapeptidomimetic compound that acts as a non-competitive antagonist of complement C5a receptor (C5aR; CD88; IC₅₀ = 240 nM) and as a low-affinity agonist for MrgX2, a GPCR, in human mast cells Shown to specifically bind to C5aR1 and not to CaR2 and C3aR. Displays a broad range of anti-inflammatory effects, both in vitro and in vivo. Shown to inhibit C5a-induced neutrophil myeloperoxidase release (IC₅₀ = 22 nM) and chemotaxis (IC₅₀ = 75 nM). Preincubation with PMX-53 (~10 nM) blocks C5a-induced Ca2+ responses in HMC-1 and RBL-2H3 cells, but does not affect C3a responses. Suppresses the growth of 4T1 mammary carcinoma tumor xenograft in mice (1 mg/kg/every 2-3 days, s.c.). Reported to diminish C5a-mediated increase in pluripotency in human embryonic stem cells in the absence of FGF2.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
C5aR

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

シーケンス

Ac-Phe-[Orn-Pro-dCha-Trp-Arg]

再構成

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

その他情報

Lillegard, K., et al. 2014. JPET.351,344.
Vadrevu, S. K., et al. 2014. Cancer Res.74, 3454.
Liang, S., et al. 2011. J. Immun.186, 869.
Woodruff, T., et al. 2005. JPET.314, 811.

法的情報

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

安全性情報

• 保管分類コード: 13 - Non Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable