| Size | Price | Stock | Qty |
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| 5mg |
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Purity: ≥98%
PD-176252 is a novel and potent non-peptide antagonist of gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1)with Ki values of 0.17 and 1.0 nM for BB1 and BB2 respectively. It inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 μM). 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.
| ln Vitro |
Neuregulin B-preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptors are effectively antagonistic to PD176252, with Kis values of 0.17 nM and 1 nM for human and rat BB1 and BB2 receptors, respectively. For the receptor, Kis are 0.66 nM and 16 nM, respectively. In addition to preventing bombesin-induced stably expressing human CHO cells, PD176252 inhibits the acidification response of human BB1 or BB2 receptors to neuregulin-B or neuregulin-C expressed in CHO cells with appKB of 4.0 nM or 13 nM. Intracellular calcium levels increased in BB1 or BB2 receptors, with appKB of 2.3 nM and 36 nM, respectively. N-Formyl peptide receptor 1/2 (FPR1/FPR2) is likewise an agonist, and PD176252 has an EC50 of 0.31 and 0.66 μM in HL-60 cells, respectively. In HL-60 cells transfected with human FPR (EC50, 0.72 ± 0.21 μM), PD176252 stimulates Ca2+ mobilization [2]. At a dosage of 1 nM, PD176252 almost completely inhibits the specific binding of 125I-gastrin-releasing peptide to NCI-H345 cells; at 1000 nM, with an IC50 of 30 nM, it almost completely blocks all specific binding. The proliferation of NCI-H345 or H1299 cells is considerably inhibited by PD176252 (10, 30 μM), with IC50 values of 7 and 5 μM, respectively [3].
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| ln Vivo |
In nude mice, PD176252 (1, 10 μg, po) efficiently suppresses the growth and proliferation of NCI-H1299 xenografts [3].
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| References |
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| Molecular Formula |
C32H36N6O5
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|---|---|
| Molecular Weight |
584.6654
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| Exact Mass |
584.275
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| CAS # |
204067-01-6
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| PubChem CID |
9829828
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
6.998
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
43
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| Complexity |
962
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| Defined Atom Stereocenter Count |
1
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| 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-]
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| InChi Key |
NNFUWNLENRUDHR-HKBQPEDESA-N
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| 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
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| Chemical Name |
1H-Indole-3-propanamide, N-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-alpha-methyl-alpha-((((4-nitrophenyl)amino)carbonyl)amino)-, (alphaS)-
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| Synonyms |
PD-176252; PD 176252; PD176252.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~115 mg/mL (~196.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5.75 mg/mL (9.83 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.75 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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