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Chemical Structure| 1628291-95-1 Chemical Structure| 1628291-95-1

Structure of HC-070
CAS No.: 1628291-95-1

Chemical Structure| 1628291-95-1

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HC-070 is a TRPC4/TRPC5 antagonist, with IC50 values of 9.3 nM for hTRPC5 and 46 nM for hTRPC4 in cells.

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Product Details of HC-070

CAS No. :1628291-95-1
Formula : C22H20Cl2N4O4
M.W : 475.32
SMILES Code : ClC1=CC=C(C=C1)CN2C(OC3=CC(Cl)=CC=C3)=NC(N(C)C(N4CCCO)=O)=C2C4=O
MDL No. :MFCD31657436

Safety of HC-070

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Th+ARC neurons 100 nM HC-070 mimicked the effects of Trpc5 deletion in Th+ARC neurons, reducing interburst intervals and eliminating prolactin-evoked long-lasting depolarization. Proc Natl Acad Sci U S A. 2019 Jul 23;116(30):15236-15243
human TRPC1/TRPC5 heteromultimer expressing cells 1.3 nM To assess the inhibitory effect of HC-070 on TRPC1/TRPC5 heteromultimers PLoS One. 2018 Jan 31;13(1):e0191225
mouse TRPC5 (mTRPC5) expressing cells 0.55 nM To assess the inhibitory effect of HC-070 on mTRPC5 PLoS One. 2018 Jan 31;13(1):e0191225
human TRPC4 (hTRPC4) expressing cells 46.0±3.9 nM To assess the inhibitory effect of HC-070 on hTRPC4 PLoS One. 2018 Jan 31;13(1):e0191225
human TRPC5 (hTRPC5) expressing cells 9.3±0.9 nM To assess the inhibitory effect of HC-070 on hTRPC5 PLoS One. 2018 Jan 31;13(1):e0191225
T-Rex-293-hTRPC4 cells 1-30 nM (Englerin A activation), 3-100 nM (GTPγS activation) To assess the inhibitory potency of HC-070 on human TRPC4. Results showed concentration-dependent inhibition of TRPC4 current with IC50 values of 0.96 nM (Englerin A) and 5.72 nM (GTPγS). Int J Mol Sci. 2023 Feb 8;24(4):3350

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Trpc5L3F1/L3F1, Trpc5-E4−/−, Trpc5-E5−/−, Th-ΔTrpc5 Bath application 100 nM Application of HC-070 mimicked the effects of Trpc5 deletion in Th+ARC neurons, reducing interburst intervals and eliminating prolactin-evoked long-lasting depolarization. Proc Natl Acad Sci U S A. 2019 Jul 23;116(30):15236-15243
Mice C57BL/6 mice Oral 1 mg/kg Single dose To assess the effect of HC-070 in a CCK-4-induced anxiety model PLoS One. 2018 Jan 31;13(1):e0191225
Rats Mechanical hypersensitivity model Intrathecal administration 19 ng Single administration HC-070 had no significant effect on netrin-1-induced mechanical hypersensitivity during both early and late phases Int J Mol Sci. 2022 Jun 14;23(12):6629
Wistar rats Conscious Wistar rats with exposed dentin Intravenous injection 0.008 nmol/g (weight) Single administration To evaluate the effect of TRPC5 channel antagonist on cold stimulation-induced dentinal sensitivity, results showed HC-070 did not significantly reduce nociceptive scores. Front Physiol. 2022 Dec 14;13:891759
Rats Visceral pain models (TNBS-induced colonic hypersensitivity and partial restraint stress model) and neuropathic pain model (chronic constriction injury model) Oral 3-30 mg/kg Single dose To evaluate the analgesic efficacy of HC-070 in rat visceral and neuropathic pain models. Results showed HC-070 significantly and dose-dependently attenuated TNBS-induced colonic hypersensitivity and had a significant anti-hypersensitivity effect in the established phase of the CCI model. Int J Mol Sci. 2023 Feb 8;24(4):3350

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.52mL

2.10mL

1.05mL

21.04mL

4.21mL

2.10mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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