An ADGRD1 agonist
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AP503

Item No. 45892

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[2-(2,4-dimethylphenoxy)acetyl]amino]-4-(4-ethyl-1-piperazinyl)-benzoic acid, methyl ester
CAS Number
767299-99-0
Synonyms
  • AP-970/43482503
Molecular Formula
C24H31N3O4
Formula Weight
425.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CC1=CC(C)=CC=C1OCC(NC2=CC(C(OC)=O)=CC=C2N3CCN(CC3)CC)=O
InChi Code
InChI=1S/C24H31N3O4/c1-5-26-10-12-27(13-11-26)21-8-7-19(24(29)30-4)15-20(21)25-23(28)16-31-22-9-6-17(2)14-18(22)3/h6-9,14-15H,5,10-13,16H2,1-4H3,(H,25,28)
InChi Key
CPGGKKARFZXWMR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AP503 is an agonist of adhesion G protein-coupled receptor D1 (ADGRD1), also known as GPR133, a G protein-coupled receptor (GPCR) involved in androgen-dependent muscle strength.1 It selectively activates Gs-signaling (EC50 = 1.2 nM) over G12- or Gi-signaling in HEK293 cells expressing ADGRD1 and does not activate the androgen receptor in a reporter assay using LNCaP cells. AP503 is also selective for ADGRD1 over a panel of 27 other adhesion GPCRs (aGPCRs) at 100 µM. It promotes tetanic contraction forces in fiber bundles isolated from mouse extensor digitorum longus tissue. Unlike the endogenous ADGRD1 agonist 5α-dihydrotestosterone (5α-DHT), AP503 does not increase the thickness of the prostatic epithelium in mice. AP503 (2 mg/kg) increases bone mass in male mice and increases cortical bone mineral density and thickness in ovariectomized mice.2

    WARNING This product is not for human or veterinary use.