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AM211 - 10mM in DMSO, high purity , CAS No.1175526-27-8(DMSO), G protein-coupled receptor 44 antagonist

COA

Grade & Purity:

10mM in DMSO

Cas Number: 1175526-27-8(DMSO)
Molecular Weight: 500.51

In stock

Item Number

A654624

Grouped product items
SKU	Size	Availability	Price	Qty
A654624-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$75.90

View related series

Compound libraries (12325) GPCR/G Protein (3172) Prostaglandin Receptor (169)

Basic Description

Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC 50 s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	ANTAGONIST
Mechanism of action	G protein-coupled receptor 44 antagonist
Product Description	AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC 50 s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In Vitro AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC 50 s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC 50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 displays high selectivity for DP2 versus other receptors in the prostanoid family, with IC 50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP of more than 100 μM. AM211 (100 μM) shows no activity at COX-1, COX-2 enzymes as well as PPAR family of nuclear receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo AM211 (1, 10, and 30 mg/kg, p.o.) dose-dependently decreases in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED 50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced pulmonary inflammation in guinea pigs. AM211 (10 mg/kg, p.o.) causes significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 4.9 nM (Human DP2), 7.8 nM (Mouse DP2), 4.9 nM (Guinea pig DP2), 10.4 nM (Rat DP2)

Associated Targets(Human)

PTGDR2 Tchem Prostaglandin D2 receptor 2 (2 Activities)

Discover Target: PTGDR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CCN(CC1=C(C=CC(=C1)C(F)(F)F)C2=C(C=CC(=C2)CC(=O)O)OC)C(=O)NCC3=CC=CC=C3
Molecular Weight	500.51

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

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