Cat. No.: HY-12158

VU0238441

고객리뷰

Based on 1 Customer Validation

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC₅₀s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.87%
CAS No.: 85511-68-8
화학식: C₁₆H₉ClF₃NO₂
분자량:339.70

보관:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

VU0238441 Chemical Structure

CAS No.: 85511-68-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

EC50: 3.2 μM (M1), 2.8 μM (M2), 2.2 μM (M3), 2.1 μM (M5) and >10 μM (M4)^[1]

All mAChR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>10 μM Compound: 2	Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	>10 μM Compound: 56	Activation of rat muscarinic M4 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of rat muscarinic M4 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
CHO	EC₅₀	2.1 μM Compound: 2	Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	2.11 μM Compound: 56	Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
CHO	EC₅₀	2.2 μM Compound: 2	Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	2.22 μM Compound: 56	Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
CHO	EC₅₀	2.8 μM Compound: 2	Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	2.84 μM Compound: 56	Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
CHO	EC₅₀	3.2 μM Compound: 2	Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	3.2 μM Compound: 56	Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]

In Vitro

VU0238441 is an analogue of VU0119498^[2].

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

Chemical Information

CAS No. 85511-68-8
Appearance Solid
분자량 339.70
화학식 C₁₆H₉ClF₃NO₂
Color Brown to red
SMILES

O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=C(C=CC=C3Cl)C1=O
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 125 mg/mL (367.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9438 mL

14.7189 mL

29.4377 mL

5 mM

0.5888 mL

2.9438 mL

5.8875 mL

10 mM

0.2944 mL

1.4719 mL

2.9438 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Thomas M Bridges, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. [Content Brief]

[2]. Thomas M Bridges, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9438 mL	14.7189 mL	29.4377 mL	73.5943 mL
	5 mM	0.5888 mL	2.9438 mL	5.8875 mL	14.7189 mL
	10 mM	0.2944 mL	1.4719 mL	2.9438 mL	7.3594 mL
	15 mM	0.1963 mL	0.9813 mL	1.9625 mL	4.9063 mL
	20 mM	0.1472 mL	0.7359 mL	1.4719 mL	3.6797 mL
	25 mM	0.1178 mL	0.5888 mL	1.1775 mL	2.9438 mL
	30 mM	0.0981 mL	0.4906 mL	0.9813 mL	2.4531 mL
	40 mM	0.0736 mL	0.3680 mL	0.7359 mL	1.8399 mL
	50 mM	0.0589 mL	0.2944 mL	0.5888 mL	1.4719 mL
	60 mM	0.0491 mL	0.2453 mL	0.4906 mL	1.2266 mL
	80 mM	0.0368 mL	0.1840 mL	0.3680 mL	0.9199 mL
	100 mM	0.0294 mL	0.1472 mL	0.2944 mL	0.7359 mL

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VU0238441

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Covalent Screening Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All mAChR Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

VU0238441

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Covalent Screening Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All mAChR Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

VU0238441 Related Classifications

HY-12158 Related Classifications