5.33683

PMX53

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

• 동의어(들): C5aR Antagonist, PMX53, Ac-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
• 실험식(Hill 표기법): C₄₇H₆₅N₁₁O₇ · xC₂HF₃O₂
• CAS Number: 219639-75-5
• Molecular Weight: 896.09 (free base basis)
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 제품명: C5aR Antagonist, PMX53,
• 분석: ≥98% (HPLC)
• Quality Level: 100
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
C5aR

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

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

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 13 - Non Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable