Thiorphan

Cat. No.: HY-W013375 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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Thiorphan is a selective NEP (neprilysin) inhibitor with an IC₅₀ of 6.9 nM.

For research use only. We do not sell to patients.

Thiorphan Chemical Structure

CAS No. : 76721-89-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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

Other Forms of Thiorphan:

Thiorphan-d₇ Get quote
Thiorphan-d₅ Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Thiorphan is a selective NEP (neprilysin) inhibitor with an IC₅₀ of 6.9 nM^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
KB 3-1	IC₅₀	4.87 mM Compound: thiorphan	Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay	[PMID: 21657271]
KB-V1	IC₅₀	2.84 mM Compound: thiorphan	Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay	[PMID: 21657271]

Molecular Weight

253.32

Formula

C₁₂H₁₅NO₃S

CAS No.

76721-89-6

Appearance

Solid

Color

White to off-white

SMILES

SCC(C(NCC(O)=O)=O)CC1=CC=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (986.89 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	3.9476 mL	19.7379 mL	39.4758 mL
5 mM	0.7895 mL	3.9476 mL	7.8952 mL
10 mM	0.3948 mL	1.9738 mL	3.9476 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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: ≥ 2.08 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (269 KB) SDS (393 KB)

COA (245 KB) HNMR (263 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Whyteside AR, Turner AJ. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Lett. 2008 Jul 9;582(16):2382-6. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.9476 mL	19.7379 mL	39.4758 mL	98.6894 mL
	5 mM	0.7895 mL	3.9476 mL	7.8952 mL	19.7379 mL
	10 mM	0.3948 mL	1.9738 mL	3.9476 mL	9.8689 mL
	15 mM	0.2632 mL	1.3159 mL	2.6317 mL	6.5793 mL
	20 mM	0.1974 mL	0.9869 mL	1.9738 mL	4.9345 mL
	25 mM	0.1579 mL	0.7895 mL	1.5790 mL	3.9476 mL
	30 mM	0.1316 mL	0.6579 mL	1.3159 mL	3.2896 mL
	40 mM	0.0987 mL	0.4934 mL	0.9869 mL	2.4672 mL
	50 mM	0.0790 mL	0.3948 mL	0.7895 mL	1.9738 mL
	60 mM	0.0658 mL	0.3290 mL	0.6579 mL	1.6448 mL
	80 mM	0.0493 mL	0.2467 mL	0.4934 mL	1.2336 mL
	100 mM	0.0395 mL	0.1974 mL	0.3948 mL	0.9869 mL

Thiorphan 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:

Thiorphan76721-89-6NeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10Inhibitorinhibitorinhibit

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