PMX-53

$240$1,320

Products Details

Product Description

– PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects[1][2][3][4][5][6].

Web ID

– HY-106178

Storage Temperature

– -80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light, under nitrogen)

Shipping

– Blue Ice

Applications

– COVID-19-immunoregulation

Molecular Formula

– C47H65N11O7

References

– [1]Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13.|[2]Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53.|[3]Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73.|[4]Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74.|[5]Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25(7):2447-55.|[6]Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74(13):3454-65.

CAS Number

– 219639-75-5

Molecular Weight

– 896.09

Compound Purity

– 98.60

SMILES

– O=C(N[C@H](C(NCCC[C@@H]1NC([C@@H](NC(C)=O)CC2=CC=CC=C2)=O)=O)CCCNC(N)=N)[C@@H](NC([C@H](NC([C@@](CCC3)([H])N3C1=O)=O)CC4CCCCC4)=O)CC5=CNC6=CC=CC=C56

Clinical Information

– No Development Reported

Research Area

– Cancer; Inflammation/Immunology; Cardiovascular Disease

Solubility

– DMSO : 200 mg/mL (ultrasonic)|H2O : 2.5 mg/mL (ultrasonic;warming;heat to 60°C)

Target

– Complement System

Pathway

– Immunology/Inflammation

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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