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	(2S)-3-(1H-indol-3-yl)-N-[[1-(5-methoxypyridin-2-yl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide \| 1H-INDOLE-3-PROPANAMIDE, N-((1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL)METHYL)-.ALPHA.-METHYL-.ALPHA.-((((4-NITROPHENYL)AMINO)CARBONYL
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(Human)

GRPR Tchem Gastrin-releasing peptide receptor (3 Activities)

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

NMBR Tchem Neuromedin-B receptor (2 Activities)

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

NMBR Tchem Neuromedin B receptor (236 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GRPR Tchem Gastrin releasing peptide receptor (289 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

RELA Tchem Nuclear factor NF-kappa-B p65 subunit (627 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

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