Cat. No.: HY-105685

SRX246

고객리뷰

Based on 1 Customer Validation

SRX246 is a potent, BBB-penetrant, highly selective vasopressin 1a (V1a) receptor antagonist (K_i=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.76%
CAS No.: 512784-93-9
화학식: C₄₂H₄₉N₅O₅
분자량:703.87

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SRX246 Chemical Structure

CAS No.: 512784-93-9

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

제품 설명

IC₅₀ & Target

V1a Receptor

All Vasopressin Receptor Isoforms :

In Vivo

SRX246 (2 mg/kg; i.v.) treatment shows that the C_max, AUC_0-∞ and t_1/2 values are 953 ng/mL, 1141 ng h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. Following an oral administration (dose 20 mg/kg), The C_max, AUC_0-∞ and t_1/2 values are 98.4 ng/mL, 624 ng h/mL and 2.38 hours, respectively^[1].

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

Animal Model:

Male Sprague-Dawley rats^[1]
Dosage:

2 mg/kg (20 mg/kg for p.o.)
Administration:

i.v. (Pharmacokinetic Analysis)
Result:

Following i.v. administration, the plasma concentration declined steadily with a half-life (t_1/2) of 6 hours. The C_max and AUC_0-∞ values are 953 ng/mL, 1141 ng ▪h/mL, 6.02 hours. Following an oral administration, the C_max, AUC_0-∞ and t_1/2 values 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 512784-93-9
Appearance Solid
분자량 703.87
화학식 C₄₂H₄₉N₅O₅
Color White to off-white
SMILES

O=C(N1CCC(N2CCCCC2)CC1)C[C@H](C(N[C@@H](C3=CC=CC=C3)C)=O)N4[C@@H]([C@H](N5[C@@H](C6=CC=CC=C6)COC5=O)C4=O)/C=C/C7=CC=CC=C7
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 100 mg/mL (142.07 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

1.4207 mL

7.1036 mL

14.2072 mL

5 mM

0.2841 mL

1.4207 mL

2.8414 mL

10 mM

0.1421 mL

0.7104 mL

1.4207 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)

In Vivo:

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

Stock Solution Working Solution

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 (3.55 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.55 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Guillon CD, et al. Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. [Content Brief]

[2]. Fabio KM, et al. Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013 Jun;102(6):2033-2043. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4207 mL	7.1036 mL	14.2072 mL	35.5179 mL
	5 mM	0.2841 mL	1.4207 mL	2.8414 mL	7.1036 mL
	10 mM	0.1421 mL	0.7104 mL	1.4207 mL	3.5518 mL
	15 mM	0.0947 mL	0.4736 mL	0.9471 mL	2.3679 mL
	20 mM	0.0710 mL	0.3552 mL	0.7104 mL	1.7759 mL
	25 mM	0.0568 mL	0.2841 mL	0.5683 mL	1.4207 mL
	30 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1839 mL
	40 mM	0.0355 mL	0.1776 mL	0.3552 mL	0.8879 mL
	50 mM	0.0284 mL	0.1421 mL	0.2841 mL	0.7104 mL
	60 mM	0.0237 mL	0.1184 mL	0.2368 mL	0.5920 mL
	80 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.4440 mL
	100 mM	0.0142 mL	0.0710 mL	0.1421 mL	0.3552 mL

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SRX246

GPCR/G Protein Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All Vasopressin Receptor Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

SRX246

GPCR/G Protein Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All Vasopressin Receptor Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

SRX246 Related Classifications

HY-105685 Related Classifications