Synonym
Baxdrostat; CIN-107; CIN107; CIN 107
IUPAC/Chemical Name
N-[(8R)-4-(1-methyl-2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)-5,6,7,8-tetrahydroisoquinolin-8-yl]propanamide
InChi Key
VDEUDSRUMNAXJG-LJQANCHMSA-N
InChi Code
InChI=1S/C22H25N3O2/c1-3-21(26)24-19-6-4-5-16-17(12-23-13-18(16)19)14-7-9-20-15(11-14)8-10-22(27)25(20)2/h7,9,11-13,19H,3-6,8,10H2,1-2H3,(H,24,26)/t19-/m1/s1
SMILES Code
CCC(N[C@@H]1CCCC2=C1C=NC=C2C3=CC4=C(N(C)C(CC4)=O)C=C3)=O
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
363.46
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: Freeman MW, Halvorsen YD, Marshall W, Pater M, Isaacsohn J, Pearce C, Murphy B, Alp N, Srivastava A, Bhatt DL, Brown MJ; BrigHTN Investigators. Phase 2 Trial of Baxdrostat for Treatment-Resistant Hypertension. N Engl J Med. 2023 Feb 2;388(5):395-405. doi: 10.1056/NEJMoa2213169. Epub 2022 Nov 7. PMID: 36342143.
2: D'Allesandro N, Hough A, Parra D. Baxdrostat for Treatment-Resistant Hypertension. N Engl J Med. 2023 May 11;388(19):1820-1821. doi: 10.1056/NEJMc2302673. PMID: 37163633.
3: Kida Y. Baxdrostat for Treatment-Resistant Hypertension. N Engl J Med. 2023 May 11;388(19):1820. doi: 10.1056/NEJMc2302673. PMID: 37163632.
4: Fisk M. Baxdrostat for Treatment-Resistant Hypertension. N Engl J Med. 2023 May 11;388(19):1821. doi: 10.1056/NEJMc2302673. PMID: 37163634.
5: Freeman MW, Halvorsen YD, Brown MJ. Baxdrostat for Treatment-Resistant Hypertension. Reply. N Engl J Med. 2023 May 11;388(19):1821-1822. doi: 10.1056/NEJMc2302673. PMID: 37163635.
6: Freeman MW, Bond M, Murphy B, Hui J, Isaacsohn J. Results from a phase 1, randomized, double-blind, multiple ascending dose study characterizing the pharmacokinetics and demonstrating the safety and selectivity of the aldosterone synthase inhibitor baxdrostat in healthy volunteers. Hypertens Res. 2023 Jan;46(1):108-118. doi: 10.1038/s41440-022-01070-4. Epub 2022 Oct 20. PMID: 36266539; PMCID: PMC9747611.
7: Forzano I, Mone P, Varzideh F, Jankauskas SS, Kansakar U, De Luca A, Santulli G. The selective aldosterone synthase inhibitor Baxdrostat significantly lowers blood pressure in patients with resistant hypertension. Front Endocrinol (Lausanne). 2022 Dec 9;13:1097968. doi: 10.3389/fendo.2022.1097968. PMID: 36568122; PMCID: PMC9780529.
8: Freeman MW, Bond M, Murphy B, Hui J, Isaacsohn J. Results From a Randomized, Open-Label, Crossover Study Evaluating the Effect of the Aldosterone Synthase Inhibitor Baxdrostat on the Pharmacokinetics of Metformin in Healthy Human Subjects. Am J Cardiovasc Drugs. 2023 May;23(3):277-286. doi: 10.1007/s40256-023-00572-x. Epub 2023 Feb 15. PMID: 36790596; PMCID: PMC9930700.
9: Ando H. Inhibition of aldosterone synthase: Does this offer advantages compared with the blockade of mineralocorticoid receptors? Hypertens Res. 2023 Apr;46(4):1056-1057. doi: 10.1038/s41440-023-01188-z. Epub 2023 Jan 18. PMID: 36653520.
10: Awosika A, Khan A, Adabanya U, Omole AE, Millis RM. Aldosterone Synthase Inhibitors and Dietary Interventions: A Combined Novel Approach for Prevention and Treatment of Cardiovascular Disease. Cureus. 2023 Mar 15;15(3):e36184. doi: 10.7759/cureus.36184. PMID: 36937127; PMCID: PMC10016316.
11: Gomez-Sanchez CE, Gomez-Sanchez EP. Aldosterone synthase inhibitors and the treatment of essential hypertension. J Clin Endocrinol Metab. 2023 Feb 6:dgad071. doi: 10.1210/clinem/dgad071. Epub ahead of print. PMID: 36740773.
