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Pico-145 (Pico145; HC608; HC-608) is a novel and potent inhibitor of TRPC1/4/5. It has much higher potency for inhibiting TRPC1/4/5 channels than previously reported agents, impressive specificity, and graded subtype selectivity within the TRPC1/4/5 channel family.
| ln Vitro |
Compound 31, C31, or pico145, is a highly effective small molecule inhibitor of the TRPC1/4/5 channel, blocking the TRPC4/TRPC5 channel that is triggered by (−)-englerin A. Pico145 inhibits TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, and TRPM8 with an IC50 of 0.349 and 1.3 nM, respectively, in cells. In HEK 293 Tet+ cells, pico145 also suppresses human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers (IC50 0.03 nM and 0.2 nM, respectively). By raising the concentration of (−)-englerin A, Pico145's efficacy can be decreased. Furthermore, Pico145 has an IC50 of 0.011 nM and efficiently blocks S1P-induced Ca2+ entry through the TRPC4-TRPC1 channel as well as the Sphingosine 1-phosphate (S1P)-activated RPC4-TRPC1 channel. Additionally, Pico145 (IC50, 0.11 nM) sensitizes Hs578T cells, an EA-sensitive cancer cell line. Both histamine-induced and store-operated Ca2+ entrance into endothelial cells are unaffected by pico145 (100 nM) [1].
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| References |
| Molecular Formula |
C23H20CLF3N4O5
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|---|---|
| Molecular Weight |
524.876914978027
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| Exact Mass |
524.107
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| CAS # |
1628287-16-0
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| PubChem CID |
85473438
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
785
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(CC2=CC=C(Cl)C=C2)C2=C(N(C)C(=O)N(CCCO)C2=O)N=C1OC1=CC=CC(OC(F)(F)F)=C1
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| InChi Key |
PRJHEJGMSOBHTO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20ClF3N4O5/c1-29-19-18(20(33)30(22(29)34)10-3-11-32)31(13-14-6-8-15(24)9-7-14)21(28-19)35-16-4-2-5-17(12-16)36-23(25,26)27/h2,4-9,12,32H,3,10-11,13H2,1H3
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| Chemical Name |
7-[(4-chlorophenyl)methyl]-1-(3-hydroxypropyl)-3-methyl-8-[3-(trifluoromethoxy)phenoxy]purine-2,6-dione
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| Synonyms |
Pico 145 Pico-145 Pico145HC608HC-608
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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 : ≥ 100 mg/mL (~190.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 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 25.0 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: ≥ 2.5 mg/mL (4.76 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 25.0 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 | 1.9052 mL | 9.5260 mL | 19.0520 mL | |
| 5 mM | 0.3810 mL | 1.9052 mL | 3.8104 mL | |
| 10 mM | 0.1905 mL | 0.9526 mL | 1.9052 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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