[CAS NO. 204067-01-6] PD176252
PRODUCTS SPECIFICATIONS [204067-01-6]
DESCRIPTION [204067-01-6]
Overview
| MDL | MFCD09971099 |
|---|---|
| Molecular Weight | 584.67 |
| Molecular Formula | C32H36N6O5 |
| SMILES | O=C(NC1=CC=C([N+]([O-])=O)C=C1)N[C@](CC2=CNC3=C2C=CC=C3)(C)C(NCC4(C5=CC=C(OC)C=N5)CCCCC4)=O |
Summary
PD176252 is a potent antagonist of neuromedin-B preferring ( BB 1 ) and gastrin-releasing peptide-preferring ( BB 2 ) receptor with K i s of 0.17 nM and 1 nM for human BB 1 and BB 2 receptors, and 0.66 nM, 16 nM for Rat BB 1 and BB 2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 ( FPR1/FPR2 ), with EC 50 s of 0.31 and 0.66 μM in HL-60 cells.
IC50 & Target
In Vitro
PD176252 is a potent antagonist of neuromedin-B preferring (BB 1 ) and gastrin-releasing peptide-preferring (BB 2 ) receptor with K i s of 0.17 nM and 1 nM for human BB 1 and BB 2 receptors, and 0.66 nM, 16 nM for Rat BB 1 and BB 2 receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB 1 or BB 2 receptors expressed in CHO cells, with the appK B s of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB 1 or BB 2 receptors, with appK B s of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC 50 s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca 2+ mobilization in HL-60 cells transfected with human FPRs (EC 50 , 0.72 ± 0.21 μM) [2] . PD176252 inhibits little specific 125 I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC 50 of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC 50 s of 7 and 5 μM [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 115 mg/mL ( 196.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7104 mL | 8.5518 mL | 17.1037 mL |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4207 mL |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7104 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 5.75 mg/mL (9.83 mM); Clear solution
References
- [1] Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.
- [2] Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90.
- [3] Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9.
