| Size | Price | Stock | Qty |
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| 5g |
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| ln Vivo |
Isosorbide (5 mg/kg; single oral dosage) significantly enhanced urine production in rats within 2 hours and remained throughout the 8-hour testing period [3]. Isosorbide (5 mg/kg; provided as a single oral dosage 30 minutes before gallium injection) significantly lowered gallium and calcium concentrations in rat urine [3]. Isosorbide (5 mg/kg; orally provided 30 minutes before gallium injection for 6 days) resulted in less renal precipitate development and less histological alterations compared with non-diuretic animals [3].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Isosorbide is rapidly absorbed after oral administration. Refer to [isosorbide mononitrate] for detailed absorption information. IN DOGS, 5.5 MILLIMOLES/KG IV CAUSED LESS SOLUTE EXCRETION THAN AN EQUIMOLAR DOSE OF MANNITOL. THE DISTRIBUTION SPACE OF LABELED ISOSORBIDE WAS 54% OF BODY WT IN INTACT & NEPHRECTOMIZED DOGS. PROXIMAL TUBULAR REABSORPTION OF ISOSORBIDE WAS PROBABLY PASSIVE. Biological Half-Life TEN NORMAL MALES RECEIVED 0.25-1.5 G/KG ISOSORBIDE. DOSE RESPONSE EFFECTS ON WATER & OSMOLAR EXCRETION STATISTICALLY SIGNIFICANT. IN 9 VOLUNTEERS, ORALLY ADMIN ISOSORBIDE APPEARED RAPIDLY IN PLASMA & EXCRETED IN URINE WITH MEAN DISAPPEARANCE HALF-LIFE OF 8 HR. ISOSORBIDE WAS RAPIDLY ABSORBED BY HUMANS FOLLOWING ORAL ADMIN & WAS EXCRETED UNCHANGED VIA KIDNEY WITH A MEAN DISAPPEARANCE T/2 OF APPROX 7 HR. IT INCREASED URINE VOLUME, CREATININE CLEARANCE, & SODIUM & CHLORIDE EXCRETION. RABBITS GIVEN ORAL DOSES OF 2 G/KG FOR 1-7 DAYS HAD EST EXCRETION T/2 OF LESS THAN 6 HR IN ALL EYE TISSUE. PEAK LEVEL & EXCRETION T/2 WAS SIMILAR IN DAMAGED & UNDAMAGED EYE TISSUE, EXCEPT IN LENS OF DAMAGED EYES IN WHICH EXCRETION T/2 WAS SHORTER THAN OF NORMAL EYES. |
| References |
[1]. Rose M, et, al. Isosorbide as a renewable platform chemical for versatile applications--quo vadis? ChemSusChem. 2012 Jan 9;5(1):167-76.
[2]. Nozawa I, et, al. Efficacy of long-term administration of isosorbide for Ménière's disease. ORL J Otorhinolaryngol Relat Spec. May-Jun 1995;57(3):135-40. [3]. Newman RA, et, al. Gallium nitrate (NSC-15200) induced toxicity in the rat: a pharmacologic, histopathologic and microanalytical investigation. Cancer. 1979 Nov;44(5):1728-40. |
| Additional Infomation |
Isosorbide is an organic molecular entity.
Isosorbide was previously available in an oral formulation for the reduction of intraocular pressure. It was approved by the FDA in 1980, but has since been discontinued. Currently, isosorbide is an organic nitrate currently available in the [isosorbide mononitrate] and [isosorbide dinitrate] forms, and is used for the prevention of angina. Refer to these drug entries for more information. Isosorbide is an organic nitrate with vasodilator activity. Isosorbide relaxes vascular smooth muscle by formation of the free radical nitric oxide (NO), which is identical to the endothelium-derived relaxing factor (EDRF). NO activates guanylyl cyclase, thereby increasing the synthesis of cGMP within smooth muscle. Elevated cGMP levels in smooth muscle activate cGMP-dependent kinase activity that leads to release of sequestered Ca2+. In turn, free Ca+ triggers dephosphorylation of light chain myosin and relaxation of peripheral arteries and veins. In addition isosorbide relaxes coronary arteries, thereby increasing the blood circulation through the ischemic area. 1,4:3,6-Dianhydro D-glucitol. Chemically inert osmotic diuretic used mainly to treat hydrocephalus; also used in glaucoma. See also: Isosorbide Dinitrate (has salt form); Isosorbide Mononitrate (has salt form). Drug Indication Isosorbide was previously indicated for temporary reduction of intraocular pressure and used to interrupt an acute glaucoma attack, however, this is not a currently approved indication. Refer to [isosorbide mononitrate] and [isosorbide dinitrate] drug entries for more isosorbide indications. FDA Label Mechanism of Action Isosorbide causes vascular relaxation, reducing systolic ophthalmic artery pressure (SOAP), systolic ocular perfusion pressure (SOPP). |
| Molecular Formula |
C6H10O4
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|---|---|
| Molecular Weight |
146.14
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| Exact Mass |
146.057
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| CAS # |
652-67-5
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| Related CAS # |
Isosorbide mononitrate;16051-77-7
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| PubChem CID |
12597
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| Appearance |
CRYSTALS
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
372.1±42.0 °C at 760 mmHg
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| Melting Point |
60-63 °C(lit.)
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| Flash Point |
178.8±27.9 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
-1.75
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
10
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| Complexity |
122
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1C([H])([H])[C@@]([H])([C@]2([H])[C@@]1([H])[C@@]([H])(C([H])([H])O2)O[H])O[H]
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| InChi Key |
KLDXJTOLSGUMSJ-JGWLITMVSA-N
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| InChi Code |
InChI=1S/C6H10O4/c7-3-1-9-6-4(8)2-10-5(3)6/h3-8H,1-2H2/t3-,4+,5-,6-/m1/s1
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| Chemical Name |
(3S,3aR,6R,6aR)-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan-3,6-diol
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| Synonyms |
Hydronol; Devicoran; Isosorbide
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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 |
| 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) |
H2O : ≥ 100 mg/mL (~684.28 mM)
DMSO : ≥ 100 mg/mL (~684.28 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (17.11 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 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 (17.11 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 25.0 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: ≥ 2.5 mg/mL (17.11 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: 150 mg/mL (1026.41 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 | 6.8428 mL | 34.2138 mL | 68.4275 mL | |
| 5 mM | 1.3686 mL | 6.8428 mL | 13.6855 mL | |
| 10 mM | 0.6843 mL | 3.4214 mL | 6.8428 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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