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PF-05105679
CAS No. 1398583-31-7
PF-05105679( PF 05105679 | PF05105679 )
Catalog No. M11666 CAS No. 1398583-31-7
PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 53 | In Stock |
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| 5MG | 87 | In Stock |
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| 10MG | 147 | In Stock |
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| 25MG | 290 | In Stock |
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| 50MG | 447 | In Stock |
|
| 100MG | 672 | In Stock |
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| 200MG | 888 | In Stock |
|
| 500MG | 1368 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePF-05105679
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NoteResearch use only, not for human use.
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Brief DescriptionPF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).
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DescriptionPF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition); displays >100-fold selectivity against a broad panel of 90 receptors, ion channels, and enzymes; demonstrates moderately potency against agonist (WS-12) and cold modalities of activation of TRPM8 in plate-based assay formats with IC50 of 181 and 480 nM, respectively, shows increased potency on voltage activation in HEK-293 cells at 12°C with IC50 of 13.8 nM; demonstrates activity in vivo in the guinea pig bladder ice water and menthol challenge tests with an IC50 of 200 nM and reduces core body temperature in the rats, and reduces pain in the cold pressor test in humans.Pain Phase 1 Clinical.
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In VitroPF-05105679 demonstrates >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily.
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In VivoPF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs. PF-05105679 (2, 20 mg/kg) has a T1/2 of 3.6 hours, a CL of 19.8 mL/min/kg, and a Vss of 6.2 L/kg for rats. Animal Model:Male beagle dogs (weight 10 to 15kg) Dosage:0.2 mg/kg (iv) or 20 mg/kg (oral gavage)(Pharmacokinetic Analysis) Administration:Iv or oral gavageResult:Had a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs.
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SynonymsPF 05105679 | PF05105679
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PathwayMembrane Transporter/Ion Channel
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TargetTRP/TRPV Channel
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RecptorTRP/TRPV Channel
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Research AreaNeurological Disease
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IndicationPain
Chemical Information
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CAS Number1398583-31-7
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Formula Weight428.463
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Molecular FormulaC26H21FN2O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 125 mg/mL (291.75 mM)
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SMILESO=C(O)C1=CC=CC(CN([C@@H](C2=CC=C(F)C=C2)C)C(C3=CC4=CC=CC=C4N=C3)=O)=C1
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Chemical Name(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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N-Oleoyl Glutamine
N-Oleoyl Glutamine (Oleoyl-L-glutamine) is an N-acyl amino acid involved in the regulation of PM20D1 and antagonizes TRPV1 of the transient receptor potential (TRP) calcium channel.
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Pyr10
Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor. Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) (IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells) .
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AMG-0347
AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.
