BILR-355

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530126

CAS#: 380378-81-4

Description: BILR-355 is a reverse transcriptase inhibitor potentially for the treatment of HIV infection. BILR 355 exhibited a nonlinear pharmacokinetic profile and low exposure after oral administration to humans

Chemical Structure

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BILR-355
CAS# 380378-81-4
Instruction

Theoretical Analysis

MedKoo Cat#: 530126
Name: BILR-355
CAS#: 380378-81-4
Chemical Formula: C25H23N5O3
Exact Mass: 441.18
Molecular Weight: 441.490
Elemental Analysis: C, 68.01; H, 5.25; N, 15.86; O, 10.87

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: BILR-355; BILR-355-BS; BILR-355BS

IUPAC/Chemical Name: 4-(2-(11-ethyl-5-methyl-6-oxo-6,11-dihydro-5H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-8-yl)ethoxy)quinoline 1-oxide

InChi Key: BEMBRAMZGVDPMH-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H23N5O3/c1-3-29-23-19(25(31)28(2)21-9-6-12-26-24(21)29)15-17(16-27-23)11-14-33-22-10-13-30(32)20-8-5-4-7-18(20)22/h4-10,12-13,15-16H,3,11,14H2,1-2H3

SMILES Code: CCN1C2=C(N(C)C(C3=CC(CCOC4=CC=[N+]([O-])C5=CC=CC=C54)=CN=C31)=O)C=CC=N2

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 441.49 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Tidjane N, Gaboury L, Couture R. Cellular localisation of the kinin B1R in the pancreas of streptozotocin-treated rat and the anti-diabetic effect of the antagonist SSR240612. Biol Chem. 2016 Apr;397(4):323-36. doi: 10.1515/hsz-2015-0230. PubMed PMID: 26841446.

2: Dias JP, Gariépy Hde B, Ongali B, Couture R. Brain kinin B1 receptor is upregulated by the oxidative stress and its activation leads to stereotypic nociceptive behavior in insulin-resistant rats. Peptides. 2015 Jul;69:118-26. doi: 10.1016/j.peptides.2015.04.022. PubMed PMID: 25959537.

3: Silva CR, Oliveira SM, Hoffmeister C, Funck V, Guerra GP, Trevisan G, Tonello R, Rossato MF, Pesquero JB, Bader M, Oliveira MS, McDougall JJ, Ferreira J. The role of kinin B1 receptor and the effect of angiotensin I-converting enzyme inhibition on acute gout attacks in rodents. Ann Rheum Dis. 2016 Jan;75(1):260-8. doi: 10.1136/annrheumdis-2014-205739. PubMed PMID: 25344431.

4: More AS, Kim HM, Khang G, Hildebrandt T, Bernlöhr C, Doods H, Vanhoutte PM, Wu D. Des-Arg9-bradykinin causes kinin B1 receptor mediated endothelium-independent contractions in endotoxin-treated porcine coronary arteries. Pharmacol Res. 2014 Dec;90:18-24. doi: 10.1016/j.phrs.2014.09.001. PubMed PMID: 25258294.

5: Nicoletti NF, Erig TC, Zanin RF, Pereira TC, Bogo MR, Campos MM, Morrone FB. Mechanisms involved in kinin-induced glioma cells proliferation: the role of ERK1/2 and PI3K/Akt pathways. J Neurooncol. 2014 Nov;120(2):235-44. doi: 10.1007/s11060-014-1549-4. PubMed PMID: 25056222.

6: Lacoste B, Tong XK, Lahjouji K, Couture R, Hamel E. Cognitive and cerebrovascular improvements following kinin B1 receptor blockade in Alzheimer's disease mice. J Neuroinflammation. 2013 May 4;10:57. doi: 10.1186/1742-2094-10-57. PubMed PMID: 23642031; PubMed Central PMCID: PMC3710240.

7: De Brito Gariepy H, Talbot S, Sénécal J, Couture R. Brain kinin B₁ receptor contributes to the onset of stereotypic nocifensive behavior in rat. Behav Brain Res. 2013 Mar 15;241:17-26. doi: 10.1016/j.bbr.2012.11.032. PubMed PMID: 23219968.

8: Marcon R, Claudino RF, Dutra RC, Bento AF, Schmidt EC, Bouzon ZL, Sordi R, Morais RL, Pesquero JB, Calixto JB. Exacerbation of DSS-induced colitis in mice lacking kinin B(1) receptors through compensatory up-regulation of kinin B(2) receptors: the role of tight junctions and intestinal homeostasis. Br J Pharmacol. 2013 Jan;168(2):389-402. doi: 10.1111/j.1476-5381.2012.02136.x. PubMed PMID: 22889120; PubMed Central PMCID: PMC3572565.

9: Dias JP, Couture R. Suppression of vascular inflammation by kinin B1 receptor antagonism in a rat model of insulin resistance. J Cardiovasc Pharmacol. 2012 Jul;60(1):61-9. doi: 10.1097/FJC.0b013e3182576277. PubMed PMID: 22494994.

10: Dias JP, Couture R. Blockade of kinin B(1) receptor reverses plasma fatty acids composition changes and body and tissue fat gain in a rat model of insulin resistance. Diabetes Obes Metab. 2012 Mar;14(3):244-53. doi: 10.1111/j.1463-1326.2011.01521.x. PubMed PMID: 22023455.

11: Pietrovski EF, Paludo KS, Mendes DA, Guimarães Fde S, Veiga SS, Buchi Dde F, Fonseca RG, Zampronio AR, Bader M, Pesquero JB, Ferreira J, Otuki MF, Cabrini DA. B1 and B2 kinin receptor participation in hyperproliferative and inflammatory skin processes in mice. J Dermatol Sci. 2011 Oct;64(1):23-30. doi: 10.1016/j.jdermsci.2011.06.016. PubMed PMID: 21840178.

12: Pouliot M, Hétu S, Lahjouji K, Couture R, Vaucher E. Modulation of retinal blood flow by kinin B₁ receptor in Streptozotocin-diabetic rats. Exp Eye Res. 2011 Jun;92(6):482-9. doi: 10.1016/j.exer.2011.03.007. PubMed PMID: 21420952.

13: Dias JP, Talbot S, Sénécal J, Carayon P, Couture R. Kinin B1 receptor enhances the oxidative stress in a rat model of insulin resistance: outcome in hypertension, allodynia and metabolic complications. PLoS One. 2010 Sep 7;5(9):e12622. doi: 10.1371/journal.pone.0012622. PubMed PMID: 20830306; PubMed Central PMCID: PMC2935380.

14: Klein J, Gonzalez J, Decramer S, Bandin F, Neau E, Salant DJ, Heeringa P, Pesquero JB, Schanstra JP, Bascands JL. Blockade of the kinin B1 receptor ameloriates glomerulonephritis. J Am Soc Nephrol. 2010 Jul;21(7):1157-64. doi: 10.1681/ASN.2009090887. PubMed PMID: 20448019; PubMed Central PMCID: PMC3152233.

15: Costa R, Manjavachi MN, Motta EM, Marotta DM, Juliano L, Torres HA, Pesquero JB, Calixto JB. The role of kinin B1 and B2 receptors in the scratching behaviour induced by proteinase-activated receptor-2 agonists in mice. Br J Pharmacol. 2010 Feb;159(4):888-97. doi: 10.1111/j.1476-5381.2009.00571.x. PubMed PMID: 20067469; PubMed Central PMCID: PMC2829214.

16: Pietrovski EF, Otuki MF, Regoli D, Bader M, Pesquero JB, Cabrini DA, Zampronio AR. The non-peptide kinin receptor antagonists FR 173657 and SSR 240612: preclinical evidence for the treatment of skin inflammation. Regul Pept. 2009 Jan 8;152(1-3):67-72. doi: 10.1016/j.regpep.2008.10.005. PubMed PMID: 18977249.

17: Klein J, Gonzalez J, Duchene J, Esposito L, Pradère JP, Neau E, Delage C, Calise D, Ahluwalia A, Carayon P, Pesquero JB, Bader M, Schanstra JP, Bascands JL. Delayed blockade of the kinin B1 receptor reduces renal inflammation and fibrosis in obstructive nephropathy. FASEB J. 2009 Jan;23(1):134-42. doi: 10.1096/fj.08-115600. PubMed PMID: 18809736.

18: Marceau F, Regoli D. Therapeutic options in inflammatory bowel disease: experimental evidence of a beneficial effect of kinin B1 receptor blockade. Br J Pharmacol. 2008 Jul;154(6):1163-5. doi: 10.1038/bjp.2008.233. PubMed PMID: 18536746; PubMed Central PMCID: PMC2483401.

19: Costa R, Marotta DM, Manjavachi MN, Fernandes ES, Lima-Garcia JF, Paszcuk AF, Quintão NL, Juliano L, Brain SD, Calixto JB. Evidence for the role of neurogenic inflammation components in trypsin-elicited scratching behaviour in mice. Br J Pharmacol. 2008 Jul;154(5):1094-103. doi: 10.1038/bjp.2008.172. PubMed PMID: 18454165; PubMed Central PMCID: PMC2451046.

20: Dias JP, Ismael MA, Pilon M, de Champlain J, Ferrari B, Carayon P, Couture R. The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 Sep;152(2):280-7. PubMed PMID: 17618300; PubMed Central PMCID: PMC1978253.