| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Treatment with Calhex 231 dramatically lowers the proliferation of cardiac fibroblasts [1]. Treatment with Calhex 231 markedly reduced the expression of MMP2/9, Col-I/III, α-SMA, and CaSR. In cardiac fibroblasts, calhex231 attenuates high glucose-induced heart fibrosis [1]. Calhex 231 has the ability to suppress the Itch (atropin-1 interacting protein 4)-ubiquitin proteasome and TGF-β1/Smads pathways. This means that it can lessen the effects of glucose-induced myocardial fibrosis, reduce collagen deposition, and stop the growth of cardiac fibroblasts [1].
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|---|---|
| ln Vivo |
In type 1 diabetes model (T1D) rats, intraperitoneal injection of Calhex 231 (4.07 mg/kg (10 µmol/kg) given daily for 12 weeks; male Wistar rats) ameliorates diabetic myocardium fibrosis [1].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: Primary neonatal rat cardiac fibroblasts (CF) Tested Concentrations: 3 µM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically diminished cardiac fibroblast proliferation. Western Blot Analysis [1] Cell Types: primary neonatal rat cardiac fibroblasts (CFs) Tested Concentrations: 3 µM Incubation Duration: 48 hrs (hours) Experimental Results: CaSR, α-SMA, Col-I/III, and MMP2/9 were Dramatically expressed Downregulation. |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (8 weeks old) injected with streptozotocin [1]
Doses: 4.07 mg/kg (10 µmol/kg) Route of Administration: intraperitoneal (ip) injection; daily; continued for 12 weeks Experimental Results: Type 1 Diabetic myocardial fibrosis is improved in diabetic rats. |
| References |
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| Molecular Formula |
C25H28CL2N2O
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|---|---|
| Molecular Weight |
443.4086
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| Exact Mass |
442.157
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| CAS # |
2387505-78-2
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| Related CAS # |
(1R,2R)-Calhex 231 hydrochloride
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| PubChem CID |
11849513
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
533
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| Defined Atom Stereocenter Count |
3
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C(N([H])[C@@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@]1([H])N([H])[C@]([H])(C([H])([H])[H])C1=C([H])C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C12)=O.Cl[H]
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| InChi Key |
KZPHZSFSFANQIS-GRFVZBLOSA-N
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| InChi Code |
InChI=1S/C25H27ClN2O.ClH/c1-17(21-10-6-8-18-7-2-3-9-22(18)21)27-23-11-4-5-12-24(23)28-25(29)19-13-15-20(26)16-14-19;/h2-3,6-10,13-17,23-24,27H,4-5,11-12H2,1H3,(H,28,29);1H/t17-,23+,24+;/m1./s1
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| Chemical Name |
4-chloro-N-[(1S,2S)-2-[[(1R)-1-naphthalen-1-ylethyl]amino]cyclohexyl]benzamide;hydrochloride
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| Synonyms |
Calhex231 HCl; Calhex-231 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~75.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.64 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2552 mL | 11.2762 mL | 22.5525 mL | |
| 5 mM | 0.4510 mL | 2.2552 mL | 4.5105 mL | |
| 10 mM | 0.2255 mL | 1.1276 mL | 2.2552 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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