| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Pilocarpine nitrate, the nitrate salt of pilocarpine, is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist used on the eye to treat elevated intraocular pressure, various types of glaucoma, and to induce miosis. It is used as eye drops to treat ocular hypertension, primary open angle glaucoma, angle closure glaucoma until surgery is feasible, and to cause the pupil to constrict after dilation.
| Targets |
M3 muscarinic receptor
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
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| Animal Protocol |
Rats: Male, aged ten weeks Two groups—exercise (EX, n = 6) and control (CN, n = 6)—of wistar rats are allocated. When the CN rats are housed in cages with the running wheel locked, the EX rats are kept in cages with a running wheel (SN-451) for 40 days, allowing them to engage in voluntary exercise. The following is the measurement of saliva produced by pilocarpine on day forty. To sum up, the rats are given anesthesia, sublingually given preweighed cotton, and then given an intraperitoneal injection of pilocarpine (0.5 mg/kg) to induce the production of saliva. And for one hour, every ten minutes, a new cotton ball is added. By deducting the initial weight from the final weight, the mass of saliva secreted is determined after the collected cotton balls are weighed once more.
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| References |
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| Additional Infomation |
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Miotics: Agents causing contraction of the pupil of the eye. Some sources use the term miotics only for the parasympathomimetics but any drug used to induce miosis is included here. Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate. |
| Molecular Formula |
C₁₁H₁₇N₃O₅
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|---|---|
| Molecular Weight |
271.27
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| Exact Mass |
271.117
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| Elemental Analysis |
C, 50.89; H, 6.08; N, 18.26; O, 19.55; S, 5.22
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| CAS # |
148-72-1
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| Related CAS # |
Pilocarpine Hydrochloride; 54-71-7; Pilocarpine; 92-13-7
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| PubChem CID |
657349
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| Appearance |
White to off-white solid powder
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| Boiling Point |
520.5ºC at 760 mmHg
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| Melting Point |
173,5-174°C
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| Flash Point |
268.6ºC
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| Vapour Pressure |
1.16E-11mmHg at 25°C
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| LogP |
1.34
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| tPSA |
110.17
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| SMILES |
CC[C@H]1[C@H](COC1=O)CC2=CN=CN2C.[N+](=O)(O)[O-]
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| InChi Key |
PRZXEPJJHQYOGF-GNAZCLTHSA-N
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| InChi Code |
InChI=1S/C11H16N2O2.HNO3/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2;2-1(3)4/h5,7-8,10H,3-4,6H2,1-2H3;(H,2,3,4)/t8-,10-;/m0./s1
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| Chemical Name |
(3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one;nitric acid
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| Synonyms |
Glycylpressin; Pilagan; Pilocarpine (nitrate); Pilocarpine mononitrate; Pilocarpini nitras; Pilocarpine nitrate salt; Pilocarpinum nitricum; Terlipressin; Remestyp
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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. |
| 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: ~250 mg/mL (~921.6 mM)
H2O: ~100 mg/mL (~368.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.67 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 (7.67 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 (7.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6864 mL | 18.4318 mL | 36.8636 mL | |
| 5 mM | 0.7373 mL | 3.6864 mL | 7.3727 mL | |
| 10 mM | 0.3686 mL | 1.8432 mL | 3.6864 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05578001 | Active Recruiting |
Drug: Pilocarpine Ophthalmic | Presbyopia Pseudophakia |
Isfahan University of Medical Sciences |
July 1, 2022 | Phase 3 |
| NCT03933631 | Recruiting | Drug: Pilocarpine Drug: Prednisolone |
Glaucoma | Montefiore Medical Center | May 1, 2019 | Phase 3 |
| NCT05564832 | Recruiting | Drug: Pilocarpine 1.25% Eye drop |
Near Vision | Shahid Beheshti University of Medical Sciences |
August 1, 2022 | Early Phase 1 |
| NCT02865473 | Recruiting | Drug: Pilocarpine | Glaucoma | Medical University of Vienna | April 20, 2016 | Not Applicable |
| NCT05352854 | Not yet recruiting | Drug: 0.5% pilocarpine eye drops |
Glaucoma Myopia |
Yune Zhao | May 1, 2022 | Not Applicable |
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