2. Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel TGF-beta/Smad
  3. COX Calcium Channel TGF-β Receptor
  4. Clonixin

Clonixin (SCH-10304) is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.

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Clonixin

Clonixin Chemische Struktur

CAS. Nr. : 17737-65-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Other Forms of Clonixin:

Clonixin Related Antibodies

Top Publications Citing Use of Products

Alle COX Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
COX COX-1 COX-2 COX-3

Alle Calcium Channel Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

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Beschreibung

Clonixin (SCH-10304) is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
Bone marrow cell EC50
> 20 3
Compound: Clonixin
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
[PMID: 27994748]
Bone marrow cell EC50
> 20 3
Compound: Clonixin
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
[PMID: 27994748]
Bone marrow cell EC50
>20 3
Compound: Clonixin
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
[PMID: 27994748]
THP-1 EC50
> 20 3
Compound: Clonixin
Induction of human THP1 cell differentiation after 4 days by flow cytometry
Induction of human THP1 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
THP-1 EC50
> 20 3
Compound: Clonixin
Induction of human THP1 cell differentiation after 4 days by flow cytometry
Induction of human THP1 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
THP-1 EC50
>20 3
Compound: Clonixin
Induction of human THP1 cell differentiation after 4 days by flow cytometry
Induction of human THP1 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
U-937 EC50
> 20 3
Compound: Clonixin
Induction of human U937 cell differentiation after 4 days by flow cytometry
Induction of human U937 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
U-937 EC50
>20 3
Compound: Clonixin
Induction of human U937 cell differentiation after 4 days by flow cytometry
Induction of human U937 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
U-937 EC50
> 20 3
Compound: Clonixin
Induction of human U937 cell differentiation after 4 days by flow cytometry
Induction of human U937 cell differentiation after 4 days by flow cytometry
[PMID: 27994748]
In Vivo

Clonixin (142 mg/kg; p.o.; daily; 7 days) administered during either the inflammatory or fibrotic phase of Bleomycin (HY-108345)-induced pulmonary fibrosis in male Sprague Dawley rats significantly reduces lung fibrosis, oxidative stress, inflammation, and improves respiratory function, with marked reductions in hydroxyproline content and Ashcroft scores[1].
Clonixin (40-120 mg/kg; i.p.; single dose) produces dose-dependent analgesia in the rat formalin nociception model[3].
Clonixin (i.p.) has an intraperitoneal LD50 of 308.0 mg/kg in Wistar rats[3].
Clonixin (i.p.) has an intraperitoneal LD50 of 266.4 mg/kg in Swiss AsW mice[3].
Clonixin (Low-intermediate-high exposure doses; i.v.; single dose) produces dose-dependent hypotension and bradycardia in rats, with reversibility limited to low doses[4].

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

Animal Model: Sprague Dawley (male, 4-6 weeks old, 200-250 g, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 142 mg/kg
Administration: p.o.; daily; 7 days (days 1-7 post-bleomycin or days 8-14 post-bleomycin)
Result: Attenuated bleomycin-induced body weight loss.
Significantly reduced lung coefficient.
Significantly reduced airway resistance.
Markedly reduced total leukocyte count in bronchoalveolar lavage fluid (BALF).
Significantly reduced lymphocyte count in BALF.
Significantly reduced monocyte count in BALF.
Reduced lung tissue malondialdehyde (MDA) levels, and restored reduced glutathione (GSH), superoxide dismutase (SOD), and catalase levels.
Significantly reduced lung hydroxyproline content.
Significantly reduced Ashcroft fibrosis score.
Reduced immunohistochemical expression of fibrotic markers α-SMA, FAP, and TNF-α in lung tissue, particularly in the days 8-14 dosing group.
Animal Model: Wistar (adult male and female; formalin-induced nociception model)[3]
Dosage: 40 mg/kg; 80 mg/kg; 120 mg/kg
Administration: i.p.; single dose
Result: Had no effect on formalin-induced nociceptive response at 40 mg/kg.
Produced significant, dose-dependent reductions in pain intensity ratings at 80 mg/kg and 120 mg/kg.
Showed non-linear temporal course of analgesia at 120 mg/kg, with pain ratings returning to control levels by end of 30-minute observation period.
Significantly reduced formalin-induced pain intensity when combined with nifedipine 5 mg/kg at 80 mg/kg.
Was approximately 10 times less potent than nifedipine and morphine in this assay.
Molekulargewicht

262.69

Formel

C13H11ClN2O2
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CN=C1NC2=CC=CC(Cl)=C2C)O
Versand

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

DMSO : 100 mg/mL (380.68 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 3.8068 mL 19.0338 mL 38.0677 mL
5 mM 0.7614 mL 3.8068 mL 7.6135 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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.
Reinheit & Dokumentation

Purity: 98.88%

SDS (393 KB)

COA (253 KB) HNMR (252 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
Verweise

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 3.8068 mL 19.0338 mL 38.0677 mL 95.1692 mL
5 mM 0.7614 mL 3.8068 mL 7.6135 mL 19.0338 mL
10 mM 0.3807 mL 1.9034 mL 3.8068 mL 9.5169 mL
15 mM 0.2538 mL 1.2689 mL 2.5378 mL 6.3446 mL
20 mM 0.1903 mL 0.9517 mL 1.9034 mL 4.7585 mL
25 mM 0.1523 mL 0.7614 mL 1.5227 mL 3.8068 mL
30 mM 0.1269 mL 0.6345 mL 1.2689 mL 3.1723 mL
40 mM 0.0952 mL 0.4758 mL 0.9517 mL 2.3792 mL
50 mM 0.0761 mL 0.3807 mL 0.7614 mL 1.9034 mL
60 mM 0.0634 mL 0.3172 mL 0.6345 mL 1.5862 mL
80 mM 0.0476 mL 0.2379 mL 0.4758 mL 1.1896 mL
100 mM 0.0381 mL 0.1903 mL 0.3807 mL 0.9517 mL
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Clonixin 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:

Clonixin17737-65-4SCH-10304SCH10304SCH 10304COXCalcium ChannelTGF-β ReceptorCyclooxygenaseCa2+ channelsCa channelsTransforming growth factor beta receptorsrat formalin nociception modelEPC LUVsSwiss AsW micevoltage-operated type-L calcium channelEPC liposome bilayerWistar ratsmale Sprague Dawley ratsbleomycin-induced pulmonary fibrosisTGF-βidiopathic pulmonary fibrosisInhibitorinhibitorinhibit

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