| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Pilocarpine HCl (Pilocarpal; NSC-5746; Ocusert; Pilocar;Pilocar SMP; Salagen; NSC5746), the hydrochloride salt of pilocarpine, is a naturally occurring and nonselective muscarinic acetylcholine receptor agonist used to treat dry mouth caused by radiotherapy in patients with head and neck cancer and in patients with Sjogren's syndrome. It is also used to produce an experimental model of epilepsy. Pilocarpine is a parasympathomimetic alkaloid extracted from the leaves of tropical American shrubs from the genus Pilocarpus. Pilocarpine acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis.
| Targets |
mAChR3/muscarinic acetylcholine receptor
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| ln Vitro |
The morphology and viability of human corneal stromal (HCS) cells are assessed using light microscopy and the MTT assay, respectively, in order to assess the cytotoxicity of pilocarpine. HCS cells exposed to Pilocarpine at concentrations between 0.625 and 20 g/L exhibit morphological abnormalities such as cellular shrinkage, cytoplasmic vacuolation, detachment from the culture matrix, and eventually death, as well as dose- and time-dependent proliferation retardation, according to morphological observations. However, there is no discernible difference between the controls and those exposed to Pilocarpine below the concentration of 0.625 g/L. The MTT assay results show that after being exposed to pilocarpine above a concentration of 0.625 g/L, the cell viability of HCS cells decreases with time and concentration (P<0.01 or 0.05), but HCS cells treated with pilocarpine below a concentration of 0.625 g/L do not significantly differ from controls[2]. With an EC50 of 2.4 mM, the partial muscarinic agonist Pilocarpine induces concentration-dependent relaxation in isolated rat tail artery segments that have been constricted with Penylephrine (10 to 200 nM)[3].
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| ln Vivo |
Examined is the saliva secreted by the exercised (EX) and control (CN) rats in response to pilocarpine. Pilocarpine induces a considerably higher amount of saliva in the EX rats than in the CN rats (P<0.01). On the other hand, the EX rats' saliva had a considerably lower Na+ concentration than the CN rats' (P<0.05)[1].
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| Cell Assay |
After HCS cells were treated with pilocarpine at a concentration from 0.15625 g/L to 20.0 g/L, their morphology and viability were detected by light microscopy and MTT assay. The membrane permeability, DNA fragmentation and ultrastructure were examined by acridine orange (AO)/ethidium bromide (EB) double-staining. DNA electrophoresis and transmission electron microscopy (TEM), cell cycle, phosphatidylserine (PS) orientation and mitochondrial transmembrane potential (MTP) were assayed by flow cytometry (FCM). And the activation of caspases was checked by ELISA[3].
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| Animal Protocol |
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| References |
[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93.
[2]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32. [3]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11. [4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52 |
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| Additional Infomation |
Pilocarpine hydrochloride is the hydrochloride salt of (+)-pilocarpine, a medication used to treat increased pressure inside the eye and dry mouth. It contains a (+)-pilocarpine.
Pilocarpine Hydrochloride is the hydrochloride salt of a natural alkaloid extracted from plants of the genus Pilocarpus with cholinergic agonist activity. As a cholinergic parasympathomimetic agent, pilocarpine predominantly binds to muscarinic receptors, thereby inducing exocrine gland secretion and stimulating smooth muscle in the bronchi, urinary tract, biliary tract, and intestinal tract. When applied topically to the eye, this agent stimulates the sphincter pupillae to contract, resulting in miosis; stimulates the ciliary muscle to contract, resulting in spasm of accomodation; and may cause a transitory rise in intraocular pressure followed by a more persistent fall due to opening of the trabecular meshwork and an increase in the outflow of aqueous humor. A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. |
| Molecular Formula |
C11H16N2O2.HCL
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| Molecular Weight |
244.72
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| Exact Mass |
208.12118
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| Elemental Analysis |
C, 53.99; H, 7.00; Cl, 14.49; N, 11.45; O, 13.08
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| CAS # |
54-71-7
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| Related CAS # |
Pilocarpine;92-13-7;Pilocarpine nitrate;148-72-1;Pilocarpine-d3 hydrochloride;1217838-88-4
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| PubChem CID |
5909
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| Appearance |
Typically exists as white to off-white solids at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
431.8±18.0 °C at 760 mmHg
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| Melting Point |
202-205 °C
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| Flash Point |
215.0±21.2 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.585
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| LogP |
-0.09
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| tPSA |
44.12
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| SMILES |
Cl[H].O1C([C@@]([H])(C([H])([H])C([H])([H])[H])[C@]([H])(C1([H])[H])C([H])([H])C1=C([H])N=C([H])N1C([H])([H])[H])=O
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| InChi Key |
RNAICSBVACLLGM-GNAZCLTHSA-N
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| InChi Code |
InChI=1S/C11H16N2O2.ClH/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2;/h5,7-8,10H,3-4,6H2,1-2H3;1H/t8-,10-;/m0./s1
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| Chemical Name |
(3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one;hydrochloride
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| Synonyms |
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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: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 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: ≥ 2.08 mg/mL (8.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 130 mg/mL (531.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0863 mL | 20.4315 mL | 40.8630 mL | |
| 5 mM | 0.8173 mL | 4.0863 mL | 8.1726 mL | |
| 10 mM | 0.4086 mL | 2.0432 mL | 4.0863 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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