Synonym
AXT914; AXT 914; AXT-914
IUPAC/Chemical Name
1-((2-bromoquinoxalin-6-yl)methyl)-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy)quinazolin-2(1H)-one
InChi Key
ALANRBCCCQEPFZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H23BrN4O2/c1-4-13-36-22-10-12-26-23(15-22)28(21-8-6-20(7-9-21)18(2)3)33-29(35)34(26)17-19-5-11-24-25(14-19)31-16-27(30)32-24/h1,5-12,14-16,18H,13,17H2,2-3H3
SMILES Code
CC(C)C1=CC=C(C=C1)C2=NC(=O)N(CC3=CC=C4N=C(Br)C=NC4=C3)C5=C2C=C(OCC#C)C=C5
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
539.43
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: John MR, Harfst E, Loeffler J, Belleli R, Mason J, Bruin GJ, Seuwen K,
Klickstein LB, Mindeholm L, Widler L, Kneissel M. AXT914 a novel, orally-active
parathyroid hormone-releasing drug in two early studies of healthy volunteers
and postmenopausal women. Bone. 2014 Jul;64:204-10. doi:
10.1016/j.bone.2014.04.015. Epub 2014 Apr 24. PMID: 24769332.
2: Lim YS, You BH, Kim HB, Lim SH, Song JG, Bae MG, Han HK, Choi YH, Choi HS. A
New Therapeutic Approach Using a Calcilytic (AXT914) for Postsurgical
Hypoparathyroidism in Female Rats. Endocrinology. 2020 Oct 1;161(10):bqaa145.
doi: 10.1210/endocr/bqaa145. PMID: 32852547.
3: Letz S, Haag C, Schulze E, Frank-Raue K, Raue F, Hofner B, Mayr B, Schöfl C.
Amino alcohol- (NPS-2143) and quinazolinone-derived calcilytics (ATF936 and
AXT914) differentially mitigate excessive signalling of calcium-sensing receptor
mutants causing Bartter syndrome Type 5 and autosomal dominant hypocalcemia.
PLoS One. 2014 Dec 15;9(12):e115178. doi: 10.1371/journal.pone.0115178. PMID:
25506941; PMCID: PMC4266668.
4: Park SY, Mun HC, Eom YS, Baek HL, Jung TS, Kim CH, Hong S, Lee S.
Identification and characterization of D410E, a novel mutation in the loop 3
domain of CASR, in autosomal dominant hypocalcemia and a therapeutic approach
using a novel calcilytic, AXT914. Clin Endocrinol (Oxf). 2013 May;78(5):687-93.
doi: 10.1111/cen.12056. PMID: 23009664.
