Rislenemdaz (Synonyms: MK-0657; CERC-301)

Name: Rislenemdaz
Brand: MedChemExpress
SKU: HY-106441A
Rating: 4.5 (0 reviews)

Cat. No.: HY-106441A Purity: 99.86%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with K_i and IC₅₀ of 8.1 nM and 3.6 nM, respectively.

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Rislenemdaz 화학구조

CAS No. : 808732-98-1

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of Rislenemdaz:

Rislenemdaz (Standard) 견적 받기

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

IC50: 3.6 nM (GluN2B)^[1]
Ki: 8.1 nM (GluN2B)^[1]

In Vitro

Rislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulating NMDA-GluN1a/GluN2B L(tk-) cells with an IC₅₀ of 3.6 nM. Rislenemdaz exhibits at least 1000× selectivity for the GluN2B receptor versus all targets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity against sigma-type receptors at 10 uM^[1].

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

In Vivo

Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P<0.001) and significantly increases swimming behavior (P<0.01 for 1, 3, and 30 mg/kg; P<0.05 for 10 mg/kg) compare to the vehicle control. Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110 nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11 uM) at the time of sampling, corresponding to approximately 5, 29, 56, 83, 94, and 98% RO, respectively, in rats. The ED₅₀ for increaing in frequency of swimming and decreasing in immobility are ~0.3 and 0.7 mg/kg, respectively, corresponding to RO of ~30 and 50%. Rislenemdaz (1, 3, 10, and 30 mg/kg) significantly increases total distance traveling (P<0.01 for 1 mg/kg; P<0.001 for 3, 10, and 30 mg/kg) compare to vehicle control over the 60 min test^[1].

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

Clinical Trial

분자량

358.41

화학식

C₁₉H₂₃FN₄O₂

CAS No.

808732-98-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@@H](F)[C@@H](CNC2=NC=CC=N2)CC1)OCC3=CC=C(C)C=C3

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (279.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7901 mL	13.9505 mL	27.9010 mL
5 mM	0.5580 mL	2.7901 mL	5.5802 mL
10 mM	0.2790 mL	1.3951 mL	2.7901 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.86%

Select Batch:

Data Sheet (272 KB) SDS (254 KB)

COA (245 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198. [Content Brief]

Cell Assay ^[1]	Rat, dog, rhesus monkey, and human plasma samples (3 mL, N=3) are incubated with 2 and 20 uM [¹⁴C] Rislenemdaz at 37°C for 30 min in a shaking water bath. Following incubation, standard ultracentrifugation methodology is used to determine the percentage of drug unbind^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[1]	Four groups of 24 rats (12/sex) are given single doses of vehicle (0.5% methylcellulose [MC] and 0.02% sodium lauryl sulfate [SLS] in deionized water) or Rislenemdaz at 10, 30 or 100 mg/kg by oral gavage at a dose volume of 10 mL/kg. Three additional groups of rats (four males and three females per group) are orally dosed in the same manner with Rislenemdaz, and 24h serial blood samples are obtained and analyzed for Rislenemdaz plasma concentrations and evaluated for systemic exposure. Young, adult, male rats are randomly assigned across the treatment groups and are administered vehicle (0.5% MC/0.02% SLS), the reference compound desipramine (20 mg/kg; a tricyclic antidepressant) dissolving in sterile water, or Rislenemdaz (0.1, 0.3, 1, 3, 10, and 30 mg/kg) suspending in 0.5% MC/0.02% SLS, twice on Day 1 (after habituation; ~24 h prior to test, and prior to dark cycle) and once on Day 2 (30 min pretest for desipramine and 45 min pretest for Rislenemdaz and vehicle)^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7901 mL	13.9505 mL	27.9010 mL	69.7525 mL
	5 mM	0.5580 mL	2.7901 mL	5.5802 mL	13.9505 mL
	10 mM	0.2790 mL	1.3951 mL	2.7901 mL	6.9753 mL
	15 mM	0.1860 mL	0.9300 mL	1.8601 mL	4.6502 mL
	20 mM	0.1395 mL	0.6975 mL	1.3951 mL	3.4876 mL
	25 mM	0.1116 mL	0.5580 mL	1.1160 mL	2.7901 mL
	30 mM	0.0930 mL	0.4650 mL	0.9300 mL	2.3251 mL
	40 mM	0.0698 mL	0.3488 mL	0.6975 mL	1.7438 mL
	50 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3951 mL
	60 mM	0.0465 mL	0.2325 mL	0.4650 mL	1.1625 mL
	80 mM	0.0349 mL	0.1744 mL	0.3488 mL	0.8719 mL
	100 mM	0.0279 mL	0.1395 mL	0.2790 mL	0.6975 mL

Rislenemdaz Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rislenemdaz808732-98-1MK-0657 CERC-301MK0657MK 0657CERC301CERC 301CERC-301iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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Rislenemdaz (Synonyms: MK-0657; CERC-301)

고객리뷰

Other Forms of Rislenemdaz:

Rislenemdaz Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All iGluR Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Rislenemdaz Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Rislenemdaz Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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