Iptakalim hydrochloride
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Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 642407-63-4
- Formula: C9H22ClN
- Molecular Weight:179.73
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Iptakalim (Ipt) hydrochloride has been shown to reverse pulmonary resistance vascular remodeling, inhibit proliferation of pulmonary arterial smooth muscle cells (PASMCs) and airway smooth muscle cells (ASMCs), as well as protect PAECs from pathological stimulation[1].
Iptakalim has an inhibitory effect on [Ca2+]cyt increase and the proliferation of pulmonary arterial SMCs induced by endothelin-1 through activation of KATP channels. Iptakalim (10 μM, 10 min) pretreatment of pulmonary arterial SMCs significantly prevents ransient ncrease of [Ca2+]cyt elicited by endothelin-1[2].
Iptakalim at he concentrations of 0.1, 1, and 10 AM lowered[3H]thymidine incorporation by 19.75±4.60% (n=10), 41.20±9.49% (n=10), and 54.74±10.11% (n=10), respectively, compared with that of cells treated only with endothelin-1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
. Iptakalim (60 mg/kg) pretreatment significantly reduced activity (LSD comparisons)[3].
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Thirty male Sprague-Dawley rats weighing 275-299 grams[3].
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Dosage:0, 10, 30, or 60 mg/kg.
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Administration:IP, 10 min before the start of a 4-min test session.
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Result:Decreased chamber activity.
Dipper entries following pretreatment with 30 and 60 mg/kg Iptakalim were significantly lower than with 0 (saline) or 10 mg/kg iptakalim pretreatment (Tukey HSD tests).
Chemical Information
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CAS No. 642407-63-4
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Appearance Solid
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Molecular Weight 179.73
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Formula C9H22ClN
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Color Yellow to orange
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SMILES
CC(C)NC(C)(C)C(C)C.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 25 mg/mL (139.10 mM; ultrasonic and warming and heat to 70°C)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (556.39 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Mengyu He, et al. Iptakalim ameliorates hypoxia-impaired human endothelial colony-forming cells proliferation, migration, and angiogenesis via Akt/eNOS pathways. Pulm Circ. 2019 Oct 18;9(3):2045894019875417. [Content Brief]
[2]. Weiping Xie, et al. Anti-proliferating effect of iptakalim, a novel KATP channel opener, in cultured rabbit pulmonary arterial smooth muscle cells. Eur J Pharmacol. 2005 Mar 28;511(2-3):81-7. [Content Brief]
[3]. S Charntikov, et al. Iptakalim attenuates self-administration and acquired goal-tracking behavior controlled by nicotine. Neuropharmacology. 2013 Dec;75:138-44. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 5.5639 mL | 27.8195 mL | 55.6390 mL | 139.0975 mL |
| 5 mM | 1.1128 mL | 5.5639 mL | 11.1278 mL | 27.8195 mL | |
| 10 mM | 0.5564 mL | 2.7820 mL | 5.5639 mL | 13.9098 mL | |
| 15 mM | 0.3709 mL | 1.8546 mL | 3.7093 mL | 9.2732 mL | |
| 20 mM | 0.2782 mL | 1.3910 mL | 2.7820 mL | 6.9549 mL | |
| 25 mM | 0.2226 mL | 1.1128 mL | 2.2256 mL | 5.5639 mL | |
| 30 mM | 0.1855 mL | 0.9273 mL | 1.8546 mL | 4.6366 mL | |
| 40 mM | 0.1391 mL | 0.6955 mL | 1.3910 mL | 3.4774 mL | |
| 50 mM | 0.1113 mL | 0.5564 mL | 1.1128 mL | 2.7820 mL | |
| 60 mM | 0.0927 mL | 0.4637 mL | 0.9273 mL | 2.3183 mL | |
| 80 mM | 0.0695 mL | 0.3477 mL | 0.6955 mL | 1.7387 mL | |
| 100 mM | 0.0556 mL | 0.2782 mL | 0.5564 mL | 1.3910 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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