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| 5mg |
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| Targets |
Rapamycin-d3 targets the same molecular target as rapamycin: the mammalian target of rapamycin (mTOR) complex 1 (mTORC1). Rapamycin is an allosteric inhibitor of mTORC1, a key regulator of cell growth, proliferation, and metabolism. By inhibiting mTORC1, rapamycin induces autophagy and has immunosuppressive and antiproliferative effects. Rapamycin-d3 is used as an internal standard for the quantification of rapamycin, and its deuterium labeling does not affect its binding properties.
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| ln Vitro |
Rapamycin-d3 exhibits the same in vitro activity as rapamycin, as it is a stable isotope-labeled analog. Rapamycin is a potent and specific inhibitor of mTOR with an IC50 of 0.1 nM in HEK293 cells. It inhibits mTORC1 signaling, leading to inhibition of cell proliferation and induction of autophagy. Rapamycin-d3 is used as an internal standard in analytical assays and does not have intrinsic biological activity beyond its role as a standard.
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| ln Vivo |
Rapamycin-d3 is not typically used in vivo as a therapeutic agent, as it is an internal standard for analytical purposes. However, rapamycin, the unlabeled compound, is used in vivo as an immunosuppressant and autophagy activator. Rapamycin has demonstrated efficacy in animal models of transplantation, cancer, and aging. Rapamycin-d3 is used in pharmacokinetic studies to quantify rapamycin levels in biological samples.
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| Enzyme Assay |
In vitro assays for Rapamycin-d3 are analytical rather than biological. The compound is used as an internal standard in LC-MS or GC-MS methods for the quantification of rapamycin. The deuterium labeling allows for differentiation between the internal standard and the analyte. These assays are used in pharmacokinetic and bioanalytical studies.
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| Cell Assay |
Rapamycin-d3 is not typically used in cellular assays as a biological agent. However, its unlabeled counterpart, rapamycin, is used in cellular assays to study mTOR signaling and autophagy. Rapamycin-d3 may be used in cellular assays for analytical purposes, such as measuring rapamycin uptake or metabolism.
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| Animal Protocol |
Rapamycin-d3 is not used in animal experiments as a therapeutic agent. However, it is used in pharmacokinetic studies in animals to quantify rapamycin levels. The compound is administered along with rapamycin, and blood and tissue samples are analyzed by LC-MS using rapamycin-d3 as an internal standard. These studies define the pharmacokinetic profile of rapamycin.
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| ADME/Pharmacokinetics |
Rapamycin-d3 has the same pharmacokinetic properties as rapamycin, as it is a stable isotope-labeled analog. Rapamycin has a molecular weight of 917.19 and is lipophilic. It is orally bioavailable and has a long half-life. Rapamycin-d3 is used as an internal standard to accurately quantify rapamycin levels in biological samples.
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| Toxicity/Toxicokinetics |
Rapamycin-d3 is considered to have the same safety profile as rapamycin. Rapamycin is generally well-tolerated at therapeutic doses but can cause adverse effects including immunosuppression, hyperlipidemia, and delayed wound healing. The compound is intended for research use as an analytical standard and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Rapamycin-d3 is a stable isotope-labeled internal standard for the quantification of rapamycin by GC- or LC-MS. It is also known as Sirolimus-d3. Rapamycin is an allosteric inhibitor of mTORC1, an autophagy activator, and an immunosuppressant. Rapamycin-d3 is available in high purity for research applications. Its use as an internal standard enables accurate pharmacokinetic and bioanalytical studies of rapamycin.
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| Molecular Formula |
C₅₁H₇₆D₃NO₁₃
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|---|---|
| Molecular Weight |
917.19
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| Exact Mass |
916.574
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| CAS # |
392711-19-2
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| Related CAS # |
Rapamycin;53123-88-9
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| PubChem CID |
5040
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| Appearance |
White to off-white solid powder
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| LogP |
6.118
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
65
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| Complexity |
1760
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
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| InChi Key |
QFJCIRLUMZQUOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3
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| Chemical Name |
1,18-dihydroxy-12-[1-(4-hydroxy-3-methoxycyclohexyl)propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
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| Synonyms |
Rapamycind3 Rapamycin d3
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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 : ~110 mg/mL (~119.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (3.00 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 27.5 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: ≥ 2.75 mg/mL (3.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0903 mL | 5.4514 mL | 10.9029 mL | |
| 5 mM | 0.2181 mL | 1.0903 mL | 2.1806 mL | |
| 10 mM | 0.1090 mL | 0.5451 mL | 1.0903 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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