BI-409306
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MedKoo CAT#: 555338

CAS#: 1189767-28-9

Description: BI-409306, also known as SUB 166499, is a potent and selective PDE9A inhibitor with an IC50 of 52 nM. PDE9A is a drug target for cognitive decline in Alzheimer's and other diseases because this enzyme reduces brain levels of the second messenger cyclic guanosine monophosphate. cGMP transduces signals by the neurotransmitters nitric oxide and glutamate.


Price and Availability

Size
Price

100mg
USD 850
1g
USD 3250
Size
Price

200mg
USD 1250
2g
USD 4650
Size
Price

500mg
USD 1950
5g
USD 7950

BI-409306, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555338
Name: BI-409306
CAS#: 1189767-28-9
Chemical Formula: C16H17N5O2
Exact Mass: 311.1382
Molecular Weight: 311.345
Elemental Analysis: C, 61.72; H, 5.50; N, 22.49; O, 10.28


Synonym: BI-409306; BI 409306; BI409306; SUB 166499; SUB-166499; SUB166499;

IUPAC/Chemical Name: 6-(pyridin-2-ylmethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

InChi Key: BZTIJCSHNVZMES-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N5O2/c22-16-13-10-18-21(12-4-7-23-8-5-12)15(13)19-14(20-16)9-11-3-1-2-6-17-11/h1-3,6,10,12H,4-5,7-9H2,(H,19,20,22)

SMILES Code: O=C1C2=C(N(C3CCOCC3)N=C2)N=C(CC4=NC=CC=C4)N1


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:
>3 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).

Harmonized System Code:
2934.99.03.00


References

1: Brown D, Nakagome K, Cordes J, Brenner R, Gründer G, Keefe RSE, Riesenberg R, Walling DP, Daniels K, Wang L, McGinniss J, Sand M. Evaluation of the Efficacy, Safety, and Tolerability of BI 409306, a Novel Phosphodiesterase 9 Inhibitor, in Cognitive Impairment in Schizophrenia: A Randomized, Double-Blind, Placebo-Controlled, Phase II Trial. Schizophr Bull. 2018 May 1. doi: 10.1093/schbul/sby049. [Epub ahead of print] PubMed PMID: 29718385.

2: Moschetti V, Kim M, Sand M, Wunderlich G, Andersen G, Feifel U, Jang IJ, Timmer W, Rosenbrock H, Boland K. The safety, tolerability and pharmacokinetics of BI 409306, a novel and potent PDE9 inhibitor: Overview of three Phase I randomised trials in healthy volunteers. Eur Neuropsychopharmacol. 2018 May;28(5):643-655. doi: 10.1016/j.euroneuro.2018.01.003. Epub 2018 Mar 19. PubMed PMID: 29567399.

3: Brown D, Daniels K, Pichereau S, Sand M. A Phase IC Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Cognitive Outcomes of BI 409306 in Patients with Mild-to-Moderate Schizophrenia. Neurol Ther. 2018 Jun;7(1):129-139. doi: 10.1007/s40120-017-0085-5. Epub 2017 Nov 24. PubMed PMID: 29177699; PubMed Central PMCID: PMC5990500.

4: Boland K, Moschetti V, Dansirikul C, Pichereau S, Gheyle L, Runge F, Zimdahl-Gelling H, Sand M. A phase I, randomized, proof-of-clinical-mechanism study assessing the pharmacokinetics and pharmacodynamics of the oral PDE9A inhibitor BI 409306 in healthy male volunteers. Hum Psychopharmacol. 2017 Jan;32(1). doi: 10.1002/hup.2569. PubMed PMID: 28120486.

5: Moschetti V, Boland K, Feifel U, Hoch A, Zimdahl-Gelling H, Sand M. First-in-human study assessing safety, tolerability and pharmacokinetics of BI 409306, a selective phosphodiesterase 9A inhibitor, in healthy males. Br J Clin Pharmacol. 2016 Nov;82(5):1315-1324. doi: 10.1111/bcp.13060. Epub 2016 Aug 22. PubMed PMID: 27378314; PubMed Central PMCID: PMC5061793.

6: Mason VL. Alzheimer's Association International Conference on Alzheimer's Disease 2015 (AAIC 2015) (July 18-23, 2015 - Washington, D.C., USA). Drugs Today (Barc). 2015 Jul;51(7):447-52. doi: 10.1358/dot.2015.51.7.2375989. PubMed PMID: 26261847.