Art. -Nr.: HY-151111

SPH3127

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SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC₅₀=0.4 nM, human plasma renin activity IC₅₀=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.

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Reinheit: 98.26%
CAS. Nr.: 1399849-02-5
Formel: C₂₂H₃₂N₆O₄
Molecular Weight:444.53

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

SPH3127 Chemical Structure

CAS. Nr.: 1399849-02-5

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Biologische Aktivität
- Beschreibung
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vivo

SPH3127 (oral administration; 0-10 mg/kg; once) shows favorable bioavailability in cynomolgus monkeys^[1].
SPH3127 (oral administration; 0-3 mg/kg; once) shows a hypotensive effect on tsukuba hypertensive mice^[1].

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

Animal Model:

Cynomolgus monkeys pretreated with a low-sodium diet and furosemide^[1]
Dosage:

0, 1, 3, and 10 mg/kg
Administration:

Oral administration; 1, 3, and 10 mg/kg; once
Result:

Inhibited plasma renin activity with the IC₅₀ value of 0.46 nM, and showed hypotensive effect.

Animal Model:

Tsukuba hypertensive mice (THM)^[1]
Dosage:

0, 0.3, 1, or 3 mg/kg
Administration:

Oral administration; 0, 0.3, 1, or 3 mg/kg; once
Result:

Exhibited a hypotensive effect on tsukuba hypertensive mice in a dose-dependent manner from 0.3 to 3 mg/kg, and showed a maximum hypotensive effect of approximately 30 mmHg at 2-3 h after administration at any dose.

Clinical Trial

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

Chemical Information

CAS. Nr. 1399849-02-5
Appearance Solid
Molecular Weight 444.53
Formel C₂₂H₃₂N₆O₄
Color Off-white to pink
SMILES

O=C(OC)NCCCN1N=C([C@H](N(C2CC2)C([C@H]3CNCCO3)=O)C)C4=CC=C(C)N=C41
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (224.96 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

2.2496 mL

11.2478 mL

22.4957 mL

5 mM

0.4499 mL

2.2496 mL

4.4991 mL

10 mM

0.2250 mL

1.1248 mL

2.2496 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Daisuke Iijima, et al. Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor. J Med Chem. 2022 Aug 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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2496 mL	11.2478 mL	22.4957 mL	56.2392 mL
	5 mM	0.4499 mL	2.2496 mL	4.4991 mL	11.2478 mL
	10 mM	0.2250 mL	1.1248 mL	2.2496 mL	5.6239 mL
	15 mM	0.1500 mL	0.7499 mL	1.4997 mL	3.7493 mL
	20 mM	0.1125 mL	0.5624 mL	1.1248 mL	2.8120 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	30 mM	0.0750 mL	0.3749 mL	0.7499 mL	1.8746 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4060 mL
	50 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL
	60 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7030 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5624 mL

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SPH3127

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound 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

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SPH3127

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound 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

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SPH3127 Related Classifications

HY-151111 Related Classifications