A nonpeptide antagonist of BB1 and BB2
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PD 176252

Item No. 42037

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αS)-N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-1H-indole-3-propanamide
CAS Number
204067-01-6
Molecular Formula
C32H36N6O5
Formula Weight
584.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
COC(C=N1)=CC=C1C2(CCCCC2)CNC([C@@](NC(NC3=CC=C([N+]([O-])=O)C=C3)=O)(CC4=CNC5=CC=CC=C54)C)=O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    PD 176252 is a nonpeptide antagonist of bombesin receptor subtype 1 (BB1) and BB2 (Kis = 0.17 and 1 nM, respectively).1 It also induces calcium mobilization in HL-60 cells expressing formyl peptide receptor 1 (FPR1) or FPR2/ALX (EC50s = 0.31 and 0.66 µM, respectively).2 PD 176252 inhibits the proliferation of C6 rat glioma cells (IC50 = 2 µM).3 Intracerebroventricular administration of PD 176252 (100 ng/animal) increases social interaction in the social interaction test in rats.4 It decreases the latency to feed in the novelty-suppressed feeding test when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ashwood, V., Brownhill, V., Higginbottom, M., et al. PD 176252 - the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg. Med. Chem. Lett. 8(18), 2589-2594 (1998).

    2. Schepetkin, I.A., Kirpotina, L.N., Khlebnikov, A.I., et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol. Pharmacol. 79(1), 77-90 (2011).

    3. Moody, T.W., Jensen, R.T., Garcia, L., et al. Nonpeptide neuromedin B receptor antagonists inhibit the proliferation of C6 cells. Eur. J. Pharmacol. 409(2), 133-142 (2000).

    4. Merali, Z., Bédard, T., Andrews, N., et al. Bombesin receptors as a novel anti-anxiety therapeutic target: BB1 receptor actions on anxiety through alterations of serotonin activity. J. Neurosci. 26(41), 10387-10396 (2006).