Cat. No.: HY-105028

Tenidap

(Synonyms: CP-66248)

고객리뷰

Based on 1 Customer Validation

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.

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Purity: 99.93%
CAS No.: 120210-48-2
화학식: C₁₄H₉ClN₂O₃S
분자량:320.75

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tenidap Chemical Structure

CAS No.: 120210-48-2

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Amount: USD 0.00

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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
- Cellular Effect
- In Vitro
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

COX-1

0.03 μM (IC₅₀)

COX-2

1.2 μM (IC₅₀)

15-LOX

MMP-8

All COX Isoforms :

All Lipoxygenase Isoforms :

All MMP Isoforms :

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.

Chemical Information

CAS No. 120210-48-2
Appearance Solid
분자량 320.75
화학식 C₁₄H₉ClN₂O₃S
Color White to yellow
SMILES

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

CP-66248
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

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)

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

3.1177 mL

15.5885 mL

31.1769 mL

5 mM

0.6235 mL

3.1177 mL

6.2354 mL

10 mM

0.3118 mL

1.5588 mL

3.1177 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (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.

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 (280 KB)
SDS (393 KB)
- 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)
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]. Blackburn Jr W D, et al. Tenidap in rheumatoid arthritis a 24‐week double‐blind comparison with hydroxychloroquine‐plus‐piroxicam, and piroxicam alone[J]. Arthritis & Rheumatism, 1995, 38(10): 1447-1456.

[2]. Breedveld F, et al. Tenidap: a novel cytokine-modulating antirheumatic drug for the treatment of rheumatoid arthritis. Scand J Rheumatol Suppl. 1994;100:31-44. [Content Brief]

[3]. Chávez JC, et al. Participation of the Cl-/HCO(3)- exchangers SLC26A3 and SLC26A6, the Cl- channel CFTR, and the regulatory factor SLC9A3R1 in mouse sperm capacitation. Biol Reprod. 2012;86(1):1-14. Published 2012 Jan 19. [Content Brief]

[4]. Liu Y, et al. Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3. Eur J Pharmacol. 2002;435(2-3):153-160. [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, 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

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Tenidap

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Potassium Channel Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

All COX Isoforms

All Lipoxygenase Isoforms

All MMP Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Tenidap Related Classifications

HY-105028 Related Classifications