PD 176252 - ≥98%(HPLC), high purity , CAS No.204067-01-6, Antagonist of BB 1 receptor;Antagonist of BB 2 receptor

Item Number

P288361

Grouped product items
SKU	Size	Availability	Price
P288361-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$96.90
P288361-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$153.90
P288361-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$279.90
P288361-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$418.90
P288361-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$629.90

GRP (BB2) and NMB (BB1) receptor antagonist

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Basic Description

Synonyms	204067-01-6\|PD 176252\|PD-176252\|PD176252\|CHEMBL405908\|1H-Indole-3-propanamide, N-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-alpha-methyl-alpha-((((4-nitrophenyl)amino)carbonyl)amino)-, (alphaS)-\|JT21Y57650\|(2S)-3-(1H-indol-3-yl)-N-[[1-(5-methoxypyridin
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Non-peptide gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1) antagonist (Kivalues are 0.17 and 1.0 nM for BB1and BB2respectively). Inhibits proliferation of rat C6 glioma cells (IC50= 2μM) and inhibits NCI-H1299 xenog
Storage Temp	Store at 2-8°C,Argon charged
Shipped In	Wet ice
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of BB 1 receptor;Antagonist of BB 2 receptor
Product Description	PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.

Associated Targets

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

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

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

Names and Identifiers

IUPAC Name	(2S)-3-(1H-indol-3-yl)-N-[[1-(5-methoxypyridin-2-yl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide
INCHI	InChI=1S/C32H36N6O5/c1-31(18-22-19-33-27-9-5-4-8-26(22)27,37-30(40)36-23-10-12-24(13-11-23)38(41)42)29(39)35-21-32(16-6-3-7-17-32)28-15-14-25(43-2)20-34-28/h4-5,8-15,19-20,33H,3,6-7,16-18,21H2,1-2H3,(H,35,39)(H2,36,37,40)/t31-/m0/s1
InChi Key	NNFUWNLENRUDHR-HKBQPEDESA-N
Canonical SMILES	CC(CC1=CNC2=CC=CC=C21)(C(=O)NCC3(CCCCC3)C4=NC=C(C=C4)OC)NC(=O)NC5=CC=C(C=C5)[N+](=O)[O-]
Isomeric SMILES	C[C@](CC1=CNC2=CC=CC=C21)(C(=O)NCC3(CCCCC3)C4=NC=C(C=C4)OC)NC(=O)NC5=CC=C(C=C5)[N+](=O)[O-]
PubChem CID	9829828
Molecular Weight	584.67