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Rimiducid

Catalog No. T14298   CAS 195514-63-7

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

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Rimiducid Chemical Structure
Rimiducid, CAS 195514-63-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 138.00
2 mg In stock $ 197.00
5 mg In stock $ 317.00
10 mg In stock $ 467.00
25 mg In stock $ 768.00
50 mg In stock $ 1,080.00
100 mg In stock $ 1,450.00
500 mg In stock $ 2,890.00
1 mL * 10 mM (in DMSO) In stock $ 386.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
Targets&IC50 FKBP:(EC50)0.1 nM
In vitro AP1903, a bivalent 'dimerizer' drug that binds FKBP and induces Fas cross-linking.?A single 2-hour treatment eliminated approximately 80% of T cells, and multiple exposures induced further apoptosis.?T cells were eliminated regardless of their proliferation state, suggesting that the AP1903/Fas system, which contains only human components, is a promising alternative to HSV-tk for treating GVHD[2].
In vivo Constitutive hGH secretion provides a convenient and accurate way to monitor the number of viable cells in vivo because hGH has a serum half-life of only ≈3 min in mice. Over 3 consecutive days, we implanted these cells i.m. into nude mice, and treated the animals i.v. with various doses of Rimiducid, and then determined serum hGH levels as a measure of the number of surviving cells. Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg[1].
Molecular Weight 1411.63
Formula C78H98N4O20
CAS No. 195514-63-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (35.42 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Clackson T, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42. 2. Thomis DC, et al. A Fas-based suicide switch in human T cells for the treatment of graft-versus-host disease. Blood. 2001 Mar 1;97(5):1249-57.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library ReFRAME Related Library Human Metabolite Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library Clinical Compound Library Drug Repurposing Compound Library

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Keywords

Rimiducid 195514-63-7 Apoptosis Metabolism Others Fatty Acid Synthase AP1903 Inhibitor FKBP AP-1903 AP 1903 inhibit FK506-binding protein inhibitor

 

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