RQ-00311651 | CAS#1257116-00-9 | T-type Ca2+ channel blocker

MedKoo Cat#: 555164 | Name: RQ-00311651

Description:

WARNING: This product is for research use only, not for human or veterinary use.

RQ-00311651 is a novel T-type Ca2+ channel blocker, in distinct rodent models for neuropathic and visceral pain.

Chemical Structure

RQ-00311651

CAS#1257116-00-9

Theoretical Analysis

MedKoo Cat#: 555164

Name: RQ-00311651

CAS#: 1257116-00-9

Chemical Formula: C19H18F3N5O2

Exact Mass: 405.1413

Molecular Weight: 405.38

Elemental Analysis: C, 56.29; H, 4.48; F, 14.06; N, 17.28; O, 7.89

Price and Availability

Size	Price	Availability	Quantity
1g	USD 6,950.00	4 Weeks
2g	USD 12,650.00	4 Weeks

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Related CAS #

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Synonym

RQ-00311651; RQ00311651; RQ 00311651;

IUPAC/Chemical Name

(1S,2S)-2-(1H-benzo[d]imidazol-2-yl)-N-((R)-1-(5-(2,2,2-trifluoroethoxy)pyrazin-2-yl)ethyl)cyclopropane-1-carboxamide

InChi Key

KXMXGSQKPDZCEW-WOPDTQHZSA-N

InChi Code

InChI=1S/C19H18F3N5O2/c1-10(15-7-24-16(8-23-15)29-9-19(20,21)22)25-18(28)12-6-11(12)17-26-13-4-2-3-5-14(13)27-17/h2-5,7-8,10-12H,6,9H2,1H3,(H,25,28)(H,26,27)/t10-,11+,12+/m1/s1

SMILES Code

O=C([C@@H]1[C@@H](C2=NC3=CC=CC=C3N2)C1)N[C@@H](C4=NC=C(OCC(F)(F)F)N=C4)C

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

RQ-00311651 is considered a state-dependent blocker of Cav3.1/Cav3.2 T channels and may serve as an orally available analgesic for treatment of neuropathic and inflammatory pain including distinct visceral pain with minimum central side effects.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

In HEK293 cells transfected with human Cav3.1 or Cav3.2, RQ-00311651 strongly suppressed T currents when tested at holding potentials of -65 ～ -60 mV, but not -80 mV, in the Cav3.1- or Cav3.2-expressing cells. RQ-00311651 also inhibited high K-induced Ca signaling in those cells.

In vitro activity:

RQ-00311651 strongly suppressed T currents when tested at holding potentials of -65 ∼ -60 mV, but not -80 mV, in the Cav3.1- or Cav3.2-expressing cells. RQ-00311651 also inhibited high K-induced Ca signaling in those cells. Reference: Pain. 2016 Aug;157(8):1655-1665. https://pubmed.ncbi.nlm.nih.gov/27023424/

In vivo activity:

RQ-00311651 may serve as an orally available analgesic for treatment of neuropathic and inflammatory pain with minimum central side effects. In mice, RQ-00311651significantly suppressed the somatic hyperalgesia and visceral pain-like nociceptive behavior/referred hyperalgesia caused by intraplantar and intracolonic administration of NaHS or Na2S, which involve the enhanced activity of Cav3.2 channels. RQ-00311651 exhibited antiallodynic or antihyperalgesic activity in rats with spinal nerve injury-induced neuropathy or in rats and mice with paclitaxel-induced neuropathy. Reference: Pain. 2016 Aug;157(8):1655-1665. https://pubmed.ncbi.nlm.nih.gov/27023424/

Preparing Stock Solutions

The following data is based on the product molecular weight 405.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Sekiguchi F, Kawara Y, Tsubota M, Kawakami E, Ozaki T, Kawaishi Y, Tomita S, Kanaoka D, Yoshida S, Ohkubo T, Kawabata A. Therapeutic potential of RQ-00311651, a novel T-type Ca2+ channel blocker, in distinct rodent models for neuropathic and visceral pain. Pain. 2016 Aug;157(8):1655-1665. doi: 10.1097/j.pain.0000000000000565. PMID: 27023424.

In vitro protocol:

In vivo protocol:

1: Sekiguchi F, Kawara Y, Tsubota M, Kawakami E, Ozaki T, Kawaishi Y, Tomita S, Kanaoka D, Yoshida S, Ohkubo T, Kawabata A. Therapeutic potential of RQ-00311651, a novel T-type Ca2+ channel blocker, in distinct rodent models for neuropathic and visceral pain. Pain. 2016 Aug;157(8):1655-65. doi: 10.1097/j.pain.0000000000000565. PubMed PMID: 27023424.