AP 20187

Cas：195514-80-8

Product Information：

AP20187 is a chemical inducer of dimerization. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice.

Chemical Formula: C82H107N5O20

Exact Mass: 1481.7509

Molecular Weight: 1482.773

Elemental Analysis: C, 66.42; H, 7.27; N, 4.72; O, 21.58

Synonym:

AP20187

AP-20187

AP 20187

Chemical Name: (1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)

InChi Key:

NSBGUMKAXUXKGI-BPNHAYRBSA-N

InChi Code:

InChI=1S/C82H107N5O20/c1-15-61(57-43-71(98-9)77(102-13)72(44-57)99-10)79(90)86-37-19-17-27-63(86)81(92)106-65(33-29-52-31-35-67(94-5)69(39-52)96-7)55-23-21-25-59(41-55)104-50-75(88)83-47-54(49-85(3)4)48-84-76(89)51-105-60-26-22-24-56(42-60)66(34-30-53-32-36-68(95-6)70(40-53)97-8)107-82(93)64-28-18-20-38-87(64)80(91)62(16-2)58-45-73(100-11)78(103-14)74(46-58)101-12/h21-26,31-32,35-36,39-46,54,61-66H,15-20,27-30,33-34,37-38,47-51H2,1-14H3,(H,83,88)(H,84,89)/t61-,62-,63-,64-,65+,66+/m0/s1

Smiles Code:

O=C([C@@H]1CCCCN1C([C@@H](CC)C2=CC(OC)=C(OC)C(OC)=C2)=O)O[C@H](CCC3=CC(OC)=C(OC)C=C3)C4=CC=CC(OCC(NCC(CNC(COC5=CC=CC([C@@H](CCC6=CC(OC)=C(OC)C=C6)OC([C@H]7N(C([C@@H](CC)C8=CC(OC)=C(OC)C(OC)=C8)=O)CCCC7)=O)=C5)=O)CN(C)C)=O)=C4

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent.

In Vivo：

Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2E-PERK mice.

References：

1. Cotugno G, Formisano P, Giacco F, Colella P, Beguinot F, Auricchio A. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Hum Gene Ther. 2007 Feb;18(2):106-17. PubMed PMID: 17328681.

2. Allocca M, Di Vicino U, Petrillo M, Carlomagno F, Domenici L, Auricchio A. Constitutive and AP20187-induced Ret activation in photoreceptors does not protect from light-induced damage. Invest Ophthalmol Vis Sci. 2007 Nov;48(11):5199-206. PubMed PMID: 17962474.

3. Alfa RW, Tuszynski MH, Blesch A. A novel inducible tyrosine kinase receptor to regulate signal transduction and neurite outgrowth. J Neurosci Res. 2009 Sep;87(12):2624-31. doi: 10.1002/jnr.22101. PubMed PMID: 19405107; PubMed Central PMCID: PMC2854653.

4. Burnett SH, Beus BJ, Avdiushko R, Qualls J, Kaplan AM, Cohen DA. Development of peritoneal adhesions in macrophage depleted mice. J Surg Res. 2006 Apr;131(2):296-301. Epub 2005 Nov 14. PubMed PMID: 16289593.

5. Zlatic SA, Grossniklaus EJ, Ryder PV, Salazar G, Mattheyses AL, Peden AA, Faundez V. Chemical-genetic disruption of clathrin function spares adaptor complex 3-dependent endosome vesicle biogenesis. Mol Biol Cell. 2013 Aug;24(15):2378-88. doi: 10.1091/mbc.E12-12-0860. Epub 2013 Jun 12. PubMed PMID: 23761069; PubMed Central PMCID: PMC3727930.

Products are for research use only. Not for human use.