2. Metabolic Enzyme/Protease
  3. Neprilysin
  4. Thiorphan

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases.

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

Thiorphan Chemical Structure

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
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10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Thiorphan:

Thiorphan Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Thiorphan

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases[1][2][3].

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]
In Vitro

Thiorphan (5 μM; 12 h) protects neurons from excitotoxic stimulation and blocks the neurodegradation of substance P (10 μM) in primary neuronal cultures exposed to 300 μM NMDA[3].

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

Thiorphan Related Antibodies

Cell Viability Assay[3]

Cell Line: Primary neuronal cultures
Concentration: 0.5-50 μM
Incubation Time: 12 h (with 300 μM NMDA for the last 1 h), then an additional 8-72 h
Result: Significantly reduced the number per unit area of pycnotic nuclei in a dose-dependent and long-lasting manner. And prevented the breakdown of SP by the cultured neurons even during an 8-h exposure, as shown by a higher relative recovery of substrtate P (SP).
In Vivo

Thiorphan (25 μg intracerebral or 50 mg/kg intraperitoneal; given as a single dose after ibotenic acid injection) reduces cortical damage and cortical caspase-3 cleavage in a mouse model of excitotoxic brain injury induced by ibotenic acid (HY-N2311), and this neuroprotective effect is still observed 12 hours after injury. This effect can be mimicked by substance P and neurokinin A, and is inhibited by NK1 and NK2 receptor blockers[3].

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

Animal Model: Newborn Swiss and C57Bl/6 mice (5-day-old)+Ibotenate-induced excitotoxic brain injury model[3]
Dosage: 25 μg
Administration: Intracerebrally (diluted in PBS containing 5% ethanol-chloroform) or 50 mg/kg intraperitoneally (diluted in PBS containing 5% ethanol-chloroform); Single injection, once, immediately after ibotenate injection .
Result: Significantly reduced the size of ibotenate-induced cortical lesions when administrated intracerebrally at a dose of 25 μg or intraperitoneally at a dose of 50 mg/kg.
Decreased cortical caspase-3 cleavage by up to 59%. This neuroprotective effect was long-lasting, and it was still observable when thiorphan was given 12 h after the insult. The effects of thiorphan were mimicked by substance P and neurokinin A.
The neuroprotective effects of thiorphan were inhibited by co-treatment with Win-51,708 (an NK1 receptor antagonist) and L-659,877 (an NK2 receptor antagonist).
Intracerebral injection of thiorphan protected grey matter against excitotoxic damage in NEP animals but not in NEP pups.
In addition, overall mortality was low in all groups, and thiorphan, substance P, neurokinin A or neurokinin B did not affect ibotenate-induced epileptic manifestations in terms of severity and frequency.
Molecular Weight

253.32

Formula

C12H15NO3S
CAS No.
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 (986.88 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 3.9475 mL 19.7376 mL 39.4753 mL
5 mM 0.7895 mL 3.9475 mL 7.8951 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9475 mL 19.7376 mL 39.4753 mL 98.6882 mL
5 mM 0.7895 mL 3.9475 mL 7.8951 mL 19.7376 mL
10 mM 0.3948 mL 1.9738 mL 3.9475 mL 9.8688 mL
15 mM 0.2632 mL 1.3158 mL 2.6317 mL 6.5792 mL
20 mM 0.1974 mL 0.9869 mL 1.9738 mL 4.9344 mL
25 mM 0.1579 mL 0.7895 mL 1.5790 mL 3.9475 mL
30 mM 0.1316 mL 0.6579 mL 1.3158 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
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Thiorphan Related Classifications

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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