| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
| 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. For detailed absorption information, please refer to [Isosorbide Mononitrate]. In dogs, intravenous administration of isosorbide at 5.5 mmol/kg resulted in less solute excretion than an equimolar dose of mannitol. In intact and nephrectomized dogs, the volume of distribution of labeled isosorbide was 54% of body weight. Proximal tubular reabsorption of isosorbide may be passive. Biological Half-Life Ten normal male dogs received isosorbide at doses of 0.25–1.5 g/kg. The dose-response effect on water and osmolar excretion was statistically significant. In 9 volunteers, isosorbide esters appeared rapidly in plasma and were excreted in urine after oral administration, with a mean disappearance half-life of 8 hours. After oral administration, isosorbide esters are rapidly absorbed by the body and excreted unchanged via the kidneys, with a mean disappearance half-life of approximately 7 hours. It increased urine output, creatinine clearance, and the excretion of sodium and chloride. In rabbits, oral administration of 2 g/kg isosorbide dimethyl ether for 1–7 days resulted in an estimated excretion half-life of less than 6 hours in all ocular tissues. Peak levels and excretion T/2 were similar in damaged and undamaged ocular tissues, but the excretion T/2 was shorter in the lens of damaged eyes than in 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 used in oral formulations to lower intraocular pressure. It was approved by the U.S. Food and Drug Administration (FDA) in 1980, but production has since ceased. Currently, isosorbide is an organic nitrate ester, available in isosorbide mononitrate and isosorbide dinitrate formulations, used for the prevention of angina. See the relevant drug entry for more information. Isosorbide is an organic nitrate ester with vasodilatory activity. Isosorbide relaxes vascular smooth muscle by generating the free radical nitric oxide (NO), which is identical to endothelial relaxing factor (EDRF). NO activates guanylate cyclase, thereby increasing the synthesis of cGMP in smooth muscle. Increased cGMP levels in smooth muscle activate cGMP-dependent protein kinase activity, leading to the release of chelated Ca2+. In turn, the free Ca2+ triggers the dephosphorylation of light chain myosin, causing dilation of peripheral arteries and veins. Furthermore, isosorbide can dilate coronary arteries, thereby increasing blood circulation in ischemic areas.
1,4:3,6-Disohydrated D-glucol. A chemically stable osmotic diuretic, primarily used to treat hydrocephalus; also used to treat glaucoma. See also: Isosorbide nitrate (salt form); Isosorbide mononitrate (salt form). Drug IndicationsIsosorbide was previously approved for temporarily lowering intraocular pressure and interrupting acute glaucoma attacks, but this indication is not currently approved. For more indications for isosorbide mononitrate and isosorbide dinitrate, see the drug entry. FDA Label Mechanism of ActionIsosorbide causes vasodilation, reducing systolic ocular artery pressure (SOAP) and 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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