1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. Chembridge-5861528

Chembridge-5861528 (Synonyms: TCS 5861528)

Cat. No.: HY-15065 Purity: 99.27%
Handling Instructions

Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC50 values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities.

For research use only. We do not sell to patients.

Chembridge-5861528 Chemical Structure

Chembridge-5861528 Chemical Structure

CAS No. : 332117-28-9

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Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 87 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 924 In-stock
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Description

Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC50 values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities[1].

IC50 & Target[1]

TRPA1

14.3 μM (IC50, allyl isothiocyanate-evoked TRPA1 response)

TRPA1

18.7 μM (IC50, 4-HNE-evoked TRPA1 response)

In Vitro

Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Chembridge-5861528 (TCS 5861528) (30 mg/kg; i.p.; twice daily for a week) significantly attenuates development of mechanical hypersensitivity in Streptozocin (HY-13753)-induced diabetes mellitus rat model[1].
Chembridge-5861528 (3 and 10 μg/rat; i.t.; once) attenuates Capsaicin (HY-10448)-induced blood flow increase in a dose-related fashion[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Hannover-Wistar rats, Streptozocin-induced diabetes mellitus model[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection, twice daily for a week
Result: Significantly attenuated development of mechanical hypersensitivity as revealed by the paw pressure test (F1,80= 31.4, P < 0.0001).
Animal Model: Male Hannover–Wistar rats (220-260 g), Capsaicin-induced neurogenic inflammation model[2]
Dosage: 0, 3, and 10 μg/rat
Administration: Intrathecal injection, 20 min before Capsaicin injection
Result: Significantly decreased the blood flow at 10 μg.
Molecular Weight

369.42

Formula

C19H23N5O3

CAS No.
SMILES

O=C1C2=C(N=CN2CC(NC3=CC=C(C(C)CC)C=C3)=O)N(C)C(N1C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (324.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7069 mL 13.5347 mL 27.0695 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (8.12 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (8.12 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
Chembridge-5861528
Cat. No.:
HY-15065
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