Pico145

SKU: orb1307876

Description

Pico145 (HC-608) is a potent and selective small-molecule inhibitor of TRPC1/4/5 channels, exhibiting sub-nanomolar IC50 values against TRPC4 and TRPC5. It is a valuable research tool for studying the roles of these channels in pain, anxiety, and cancer in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1628287-16-0
MW	524.88
Purity	99.06% (May vary between batches)
Formula	C₂₃H₂₀ClF₃N₄O₅
SMILES	Cn1c2nc(Oc3cccc(OC(F)(F)F)c3)n(Cc3ccc(Cl)cc3)c2c(=O)n(CCCO)c1=O
Target	TRP/TRPV Channel
Solubility	DMSO:99 mg/mL (188.61 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.29 mM)

Bioactivity

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Target IC50

TRPC5:1.3 nM (cell assay)|TRPC4:0.349 nM (cell assay)|TRPC5-TRPC1:0.2 nM (cell assay)|TRPC4-TRPC1:0.03 nM (cell assay)

In Vitro

Pico145 is a remarkable small-molecule inhibitor of TRPC1/4/5 channels. Pico145 displays no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 inhibits ( )-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells). Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM, and 0.2 nM, respectively). Pico145 effectively inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P) and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels (IC50: 0.011 nM). The potency of Pico145 can be reduced by increased ( )-englerin A concentration. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, HC 608, HC608, HC-608, inhibit, Pico 145, Pico145, Pico-145, Transient receptor potential channels, TRP Channel, TRPC4, TRPC4, cell assay, TRPC4-TRPC1, TRPC4-TRPC1, cell assay, TRPC5, TRPC5, cell assay, TRPC5-TRPC1, TRPC5-TRPC1, cell assay, TRPChannel, TRPV Channel, TRPVChannel

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Compound Identifiers

PubChem CID

85473438 ↗

Key Properties

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No computed properties available.

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Pico145 (orb1307876)

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Purity:	>98% (HPLC)
CAS Number:	1628287-16-0
MW:	524.9
Formula:	C₂₃H₂₀ClF₃N₄O₅

Pico145

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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