| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
PF-5190457 is a novel, potent, orally available and selective ghrelin receptor inverse agonist with a pKi of 8.36. PF-5190457 stimulates human islets with glucose to effectively increase insulin secretion. The ghrelin receptor pharmacology and off-target selectivity of PF-5190457 are better balanced. Clinical trials involving humans were initiated for PF-5190457 due to its encouraging safety and pharmacological profile.
| Targets |
Humnan ghrelin receptor ( pKi = 8.36 )
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|---|---|
| ln Vitro |
PF-5190457 possesses an optimal ratio between off-target selectivity and ghrelin receptor pharmacology[1].
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| ln Vivo |
PF-5190457 has strong increases in glucose-stimulated insulin secretion in human whole and dispersed islets, along with excellent selectivity[1].
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| References | |
| Additional Infomation |
PF-5190457 is under investigation in clinical trial NCT01522807 (A Study Of Three PF-05190457 Formulations In Healthy Volunteers).
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| Molecular Formula |
C29H32N6OS
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|---|---|
| Molecular Weight |
512.668984413147
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| Exact Mass |
512.235
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| Elemental Analysis |
C, 67.94; H, 6.29; N, 16.39; O, 3.12; S, 6.25
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| CAS # |
1334782-79-4
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| PubChem CID |
58438464
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.757
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
842
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S1C(C)=CN2C1=NC(=C2)CC(N1CCC2(CC1)CN([C@H]1C3C=CC(C4C=C(C)N=CN=4)=CC=3CC1)C2)=O
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| InChi Key |
ZIUDADZJCKGWKR-AREMUKBSSA-N
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| InChi Code |
InChI=1S/C29H32N6OS/c1-19-11-25(31-18-30-19)22-3-5-24-21(12-22)4-6-26(24)35-16-29(17-35)7-9-33(10-8-29)27(36)13-23-15-34-14-20(2)37-28(34)32-23/h3,5,11-12,14-15,18,26H,4,6-10,13,16-17H2,1-2H3/t26-/m1/s1
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| Chemical Name |
2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone
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| Synonyms |
PF5190457; PF-05190457; PF-5190457; PF 5190457; PF05190457; PF 05190457
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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 |
| 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: ~250 mg/mL (~487.6 mM)
Ethanol: ~100 mg/mL (~195.1 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear EtOH 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: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 2.08 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9506 mL | 9.7529 mL | 19.5057 mL | |
| 5 mM | 0.3901 mL | 1.9506 mL | 3.9011 mL | |
| 10 mM | 0.1951 mL | 0.9753 mL | 1.9506 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01522807 | Completed | Drug: PF-05190457 | Diabetes Mellitus, Type 2 | Pfizer | September 2011 | Phase 1 |
| NCT01247896 | Completed | Drug: PF-05190457 | Diabetes Mellitus, Type II | Pfizer | December 2010 | Phase 1 |
| NCT02039349 | Completed | Drug: PF-05190457 | Alcoholism Alcohol Dependence |
National Institute on Alcohol Abuse and Alcoholism (NIAAA) |
January 3, 2014 | Phase 1 |
| NCT01372163 | Terminated | Drug: PF-05190457 or Placebo | Diabetes Mellitus, Type 2 | Pfizer | July 2011 | Phase 1 |
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