| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 5g |
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| 10g |
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| 25g | |||
| Other Sizes |
Pidotimod (PGT-1A) is an oral immunomodulator/immunostimulant and a synthetic dipeptide with immunomodulatory properties against adaptive and the innate immune systems. Also able to increase the concentration of salivary IgA directed against bacteria. Pidotimod increases macrophage activity and humoral immune functions, and can be used for chronic bronchitis, chronic obstructive pulmonary disease (COPD), bronchiectasis, and chronic idiopathic urticaria.
| ln Vivo |
Pidotimod (oral gavage; 800 mg/kg; 12 months) was found to be harmless to rats and 600 mg/kg to dogs in animal toxicology investigations. Pidotimod has no effect on embryonic and fetal development in rats (up to 1000 mg/kg/day), nor does it have any teratogenic effects when administered orally at 600 mg/kg or intravenously at 1000 mg/kg. It also has no effect on the perinatal or postnatal phase. no harmful repercussions after childbirth. Rat (orally 600 mg/kg) [1]. Pidotimod (ip; 200 mg/kg; 5 days) increased the activity of natural killer (NK) cells, the reaction to concanavalin A (ConA), and the proliferation of leukocytes in response to mitogens like interleukin 2. IL-2)[2]. In methylprednisolone-induced immunosuppressed mice, pidotimod (ip; 10-100 mg/kg) markedly boosts macrophage superoxygenation and normalizes the depletion of peritoneal macrophage numbers [2].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Bioavailability: 45%. 95% of the intravenously administered dose is excreted unchanged in the urine. Biological Half-Life Half-life: 4 hours. |
| References |
[1]. Ashok Mahashur, et al. Pidotimod: In-depth review of current evidence. Lung India
[2]. Ning Zhao, et al. Pidotimod: a review of its pharmacological features and clinical effectiveness in respiratory tract infections. Expert Rev Anti Infect Ther. 2019 Oct;17(10):803-818. |
| Additional Infomation |
(4R)-3-[oxo-[(2S)-5-oxo-2-pyrrolyl]methyl]-4-thiazolidinic acid is a peptide. Pidotimod is a synthetic dipeptide with immunomodulatory properties. Drug Indications: For the treatment of cell-mediated immunosuppression caused by respiratory or urinary tract infections, as an immunostimulatory therapy. Mechanism of Action: Pidotimod inhibits tumor necrosis factor-α (TNF-α)-induced increased phosphorylation of extracellular signal-regulated kinase (ERK). It also increases the expression and translocation of nuclear factor κB (NFκB) to the nucleus. It is these two regulatory effects on the ERK and NFκB signaling pathways that are thought to lead to the increased expression of Toll-like receptors induced by pidotimod. Pidotimod promotes the maturation of dendritic cells responsible for presenting antigens to naïve Th cells. It also appears to increase the number of these cells differentiating into Th1 cells, which are thought to mediate immune responses against pathogens such as bacteria and viruses. Finally, pidotimod also appears to enhance antigen-specific antibody titers and cytotoxic responses following antigen exposure. However, the exact mechanisms and timelines leading to these effects remain unclear.
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| Molecular Formula |
C9H12N2O4S
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|---|---|
| Molecular Weight |
244.2676
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| Exact Mass |
244.051
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| Elemental Analysis |
C, 44.25; H, 4.95; N, 11.47; O, 26.20; S, 13.13
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| CAS # |
121808-62-6
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| PubChem CID |
65944
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| Appearance |
Solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
663.0±55.0 °C at 760 mmHg
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| Melting Point |
194-198ºC (dec.)
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| Flash Point |
354.8±31.5 °C
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| Vapour Pressure |
0.0±4.3 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
-2.38
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
|
| Complexity |
346
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
S1C([H])([H])N(C([C@]2([H])C([H])([H])C([H])([H])C(N2[H])=O)=O)[C@]([H])(C(=O)O[H])C1([H])[H]
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| InChi Key |
UUTKICFRNVKFRG-WDSKDSINSA-N
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| InChi Code |
InChI=1S/C9H12N2O4S/c12-7-2-1-5(10-7)8(13)11-4-16-3-6(11)9(14)15/h5-6H,1-4H2,(H,10,12)(H,14,15)/t5-,6-/m0/s1
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| Chemical Name |
(R)-3-((S)-5-Oxopyrrolidine-2-carbonyl)thiazolidine-4-carboxylic acid
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| Synonyms |
Pidotomod; PGT/1A; PGT 1A; PGT1A; PGT-1A;
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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) |
DMSO : ~100 mg/mL (~409.38 mM)
H2O : ~25 mg/mL (~102.35 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.23 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 (10.23 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 (10.23 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: 14.29 mg/mL (58.50 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0938 mL | 20.4692 mL | 40.9383 mL | |
| 5 mM | 0.8188 mL | 4.0938 mL | 8.1877 mL | |
| 10 mM | 0.4094 mL | 2.0469 mL | 4.0938 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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