2. Immunology/Inflammation Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. COX Lipoxygenase Potassium Channel MMP
  4. Tenidap

Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC50=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis.

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

Tenidap

Tenidap Chemical Structure

CAS No. : 120210-48-2

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 Customer Validation

Other Forms of Tenidap:

Tenidap Related Antibodies

Top Publications Citing Use of Products

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

View All Lipoxygenase Isoform Specific Products:

View All Isoforms
5-LOX 12-LOX 15-LOX

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC50=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis[1][2][3][4].

IC50 & Target

COX-1

0.03 μM (IC50)

COX-2

1.2 μM (IC50)

15-LOX

 

MMP-8

 

Cellular Effect
Cell Line Type Value Description References
RBL-1 IC50
0.01 μM
Compound: 2 (tenidap)
In vitro inhibition of Prostaglandin G/H synthase pathway in rat basophilic leukemia (RBL-1) cells
In vitro inhibition of Prostaglandin G/H synthase pathway in rat basophilic leukemia (RBL-1) cells
[PMID: 2113951]
RBL-1 IC50
9 μM
Compound: 2 (tenidap)
In vitro inhibition of 5-lipoxygenase pathway in rat basophilic leukemia (RBL-1) cells
In vitro inhibition of 5-lipoxygenase pathway in rat basophilic leukemia (RBL-1) cells
[PMID: 2113951]
THP-1 IC50
16 μM
Compound: Tenidap
In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
[PMID: 10821716]
In Vitro

Tenidap potently inhibits leukotriene B4 and prostanoid synthesis in human polymorphonuclear leukocytes in vitro[1].
Tenidap (20 μg/mL; therapeutic concentrations) reduces IL-1β receptor expression in normal and osteoarthritic human chondrocytes, and potently suppresses IL-1β-induced collagenase and stromelysin synthesis and mRNA levels in these cells[2].
Tenidap potently inhibits bone resorption induced by parathyroid hormone, vitamin D3, IL-1α, TNF-α, and prostaglandin E2 in in vitro bone cultures, with effects independent of prostaglandin synthesis suppression[2].
Tenidap inhibits vitamin D3-induced CD14 expression, partially reverses reduced 3H-thymidine uptake, and suppresses early-stage IFN-γ-stimulated complement C2 production in HL-60 myelomonocytic cells, with no effect on C2 production in differentiated cells[2].
Tenidap potently inhibits adhesion of neutrophils, eosinophils, monocytes, and T cells to endothelial cells in in vitro adhesion assays, including IL-1-stimulated models[2].
Tenidap (0.01-10 μM; 50 min) potently and dose-dependently enhances Ba2+-sensitive 86Rb+ efflux through hKir2.3 channels in CHO cells with an EC50 of 402 nM[4].
Tenidap (30 μM; 5 min, not specified) is selective for hKir2.3 channels, as it has little or no effect on hKv1.5, μ1 Na+, or hKir2.1 channels in stably transfected cells[4].

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

Tenidap Related Antibodies
Molecular Weight

320.75

Formula

C14H9ClN2O3S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O/C(C1=CC=CS1)=C2C3=C(C=CC(Cl)=C3)N(C(N)=O)C/2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (77.94 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 3.1177 mL 15.5885 mL 31.1769 mL
5 mM 0.6235 mL 3.1177 mL 6.2354 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. 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: 2.5 mg/mL (7.79 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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).
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. 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 3.1177 mL 15.5885 mL 31.1769 mL 77.9423 mL
5 mM 0.6235 mL 3.1177 mL 6.2354 mL 15.5885 mL
10 mM 0.3118 mL 1.5588 mL 3.1177 mL 7.7942 mL
15 mM 0.2078 mL 1.0392 mL 2.0785 mL 5.1962 mL
20 mM 0.1559 mL 0.7794 mL 1.5588 mL 3.8971 mL
25 mM 0.1247 mL 0.6235 mL 1.2471 mL 3.1177 mL
30 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5981 mL
40 mM 0.0779 mL 0.3897 mL 0.7794 mL 1.9486 mL
50 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
60 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Tenidap 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:

Tenidap120210-48-2CP-66248CP66248CP 66248COXLipoxygenasePotassium ChannelMMPCyclooxygenaseLOXKcsAMatrix metalloproteinasestumor necrosis factor-alphamouse spermhKir2.3 channelhuman hepatoma (Hep 3B) cellschondrocytesinterleukin-1human polymorphonuclear leukocytesrheumatoid arthritis5-lipoxygenasecyclooxygenaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tenidap
Cat. No.:
HY-105028
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.