Rapamycin

 Cat.No.£ºIC-011768

Product Information

Biological Activity

Rapamycin was used as a kind of original antifungal antibiotic, which is produced by Streptomyces hygroscopicus. Now it has been used in the prevention of transplant rejection because of its immunosuppressive effect.  It also exhibits activity against several transplantable tumors and slightly activity to inactive against leukemias. The immunosuppressive effect of Rapamycin is exerted by inhibiting the activation and proliferation of T cells. Rapamycin binds to FK-binding protein 12 (FKBP12) and forms the rapamycin-FKBP12 complex, which regulates an enzyme that plays an important role in the progression of the cell cycle.

Rapamycin (Sirolimus,Rapamune)is an inhibitor of mTOR.The mammalian target of rapamycin (mTOR) is a kinase responsible for mitogen-induced cell proliferation/survival signaling.In vitro, rapamycin inhibited the proliferation of primary bone marrow cells induced by IL-3, GM-CSF, KL, or a complex mixture of factors present in cell-conditioned media.

Cell experiment [1]:

Cell lines£º

Hepatocyte growth factor (HGF)-induced lens epithelial cells (LECs)

Preparation method£º

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ¡ãC for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20¡ãC for several months.

Reacting condition£º

0~80nM£¬10 ng/ml, 72h

Applications£º

Using cell proliferation, cell viability and flow cytometric apoptosis assays, we found that rapamycin potently not only suppressed proliferation but also induced the apoptosis of LECs in a dose-dependent manner under HGF administration. Further investigation of the underlying mechanism using siRNA transfection revealed that rapamycin could promote apoptosis of LECs via inhibiting HGF-induced phosphorylation of AKT/mTOR, ERK and JAK2/STAT3 signaling molecules. Moreover, the forced expression of AKT, ERK and STAT3 could induce a significant suppression of apoptosis in these cells after treatment of rapamycin.

Animal experiment [2]:

Animal models£º

Ndufs4(−/−) mice

Dosage form£º

8 mg/kg every other day, intraperitoneal injection

Application£º

Rapamycin, a specific inhibitor of the mechanistic target of rapamycin (mTOR) signaling pathway, robustly enhances survival and attenuates disease progression in a mouse model of Leigh syndrome. Administration of rapamycin to these mice, which are deficient in the mitochondrial respiratory chain subunit Ndufs4 [NADH dehydrogenase (ubiquinone) Fe-S protein 4], delays onset of neurological symptoms, reduces neuroinflammation, and prevents brain lesions. Although the precise mechanism of rescue remains to be determined, rapamycin induces a metabolic shift toward amino acid catabolism and away from glycolysis, alleviating the buildup of glycolytic intermediates. This therapeutic strategy may prove relevant for a broad range of mitochondrial diseases.

Other notes£º

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Quantity

Price($)

Price($)

Availability

50mg

$180.00

€150.00

In stock

500mg

$450.00

€375.00

In stock

1g

$620.00

€516.67

In stock

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

914.18

Formula

C51H79NO13

CAS Number

53123-88-9

Purity

>98%

Solubility

45.71mg/mL in DMSO

Storage

at -20¡ãC

References Information

[1] Tian F, Dong L, Zhou Y et al. Rapamycin-Induced Apoptosis in HGF-Stimulated Lens Epithelial Cells by AKT/mTOR, ERK and JAK2/STAT3 Pathways. Int J Mol Sci. 2014 Aug 11;15(8):13833-48..

[2] Johnson SC1, Yanos ME, Kayser EB et al. mTOR inhibition alleviates mitochondrial disease in a mouse model of Leigh syndrome. Science. 2013 Dec 20;342(6165):1524-8.

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