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MedKoo Cat#: 532358 | Name: NNC269100
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Description:

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

NNC269100 is a somatostatin sst4 receptor agonist that displays > 100-fold selectivity over sst2 receptors (Ki values are 6 and 621 nM for sst4 and sst2 receptors respectively). NNC269100 potently inhibits forskolin-induced cAMP accumulation (EC50 = 26 nM).

Chemical Structure

NNC269100
NNC269100
CAS#199522-35-5

Theoretical Analysis

MedKoo Cat#: 532358

Name: NNC269100

CAS#: 199522-35-5

Chemical Formula: C22H25BrCl2N6S

Exact Mass: 554.0422

Molecular Weight: 556.35

Elemental Analysis: C, 47.50; H, 4.53; Br, 14.36; Cl, 12.74; N, 15.11; S, 5.76

Price and Availability

Size Price Availability Quantity
10mg USD 360.00
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Related CAS #
No Data
Synonym
NNC269100; NNC 269100; NNC-269100.
IUPAC/Chemical Name
1-(3-(1H-imidazol-5-yl)propyl)-3-(3-((5-bromopyridin-2-yl)(3,4-dichlorobenzyl)amino)propyl)thiourea
InChi Key
UREJDUPKGMFJRU-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H25BrCl2N6S/c23-17-5-7-21(29-12-17)31(14-16-4-6-19(24)20(25)11-16)10-2-9-28-22(32)27-8-1-3-18-13-26-15-30-18/h4-7,11-13,15H,1-3,8-10,14H2,(H,26,30)(H2,27,28,32)
SMILES Code
S=C(NCCCC1=CN=CN1)NCCCN(C2=NC=C(Br)C=C2)CC3=CC=C(Cl)C(Cl)=C3
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
NNC269100 is a somatostatin sst4 receptor agonist.
In vitro activity:
Addition of NNC (NNC 26-9100) decreased the LPS-induce lactate dehydrogenase release, had no effect in the alamar blue assay, decreased nitrite release and decreased cytosolic calcium. In the absence of LPS, NNC increased uptake of FITC-tagged Aβ1-42. These data demonstrate that NNC treatment decreases nitrosative stress and microglia cell damage during LPS-induced activation and enhances phagocytosis of Aβ1-42 during non-inflammatory conditions. Reference: PLoS One. 2021 Jul 8;16(7):e0254242. https://pubmed.ncbi.nlm.nih.gov/34237100/
In vivo activity:
Mice were administered NNC 26-9100 (0.2 µg, i.c.v.) or vehicle control, with cortical and subcortical brain tissue collected at 6 h and 24 h post-treatment. At 6 h, NNC 26-9100 treatment decreased cortical expression of cluster of differentiation-33 (Cd33) by 25%, while increasing cortical and subcortical macrophage scavenger receptor-1 (Msr1) by 1.8 and 2.0-fold, respectively. At 24 h, NNC 26-9100 treatment increased the cortical expression of Sstr4 (4.9-fold), Aβ-degrading enzymes neprilysin (9.3-fold) and insulin degrading enzyme (14.8-fold), and the antioxidant catalase (3.6-fold). Reference: Neurochem Res. 2019 Nov;44(11):2670-2680. https://pubmed.ncbi.nlm.nih.gov/31630317/
Solvent mg/mL mM
Solubility
DMSO 27.8 50.00
Ethanol 27.8 50.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 556.35 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:
1. Schober J, Polina J, Walters F, Scott N, Lodholz E, Crider A, Sandoval K, Witt K. NNC 26-9100 increases Aβ1-42 phagocytosis, inhibits nitric oxide production and decreases calcium in BV2 microglia cells. PLoS One. 2021 Jul 8;16(7):e0254242. doi: 10.1371/journal.pone.0254242. PMID: 34237100; PMCID: PMC8266108. 2. Sandoval K, Umbaugh D, House A, Crider A, Witt K. Somatostatin Receptor Subtype-4 Regulates mRNA Expression of Amyloid-Beta Degrading Enzymes and Microglia Mediators of Phagocytosis in Brains of 3xTg-AD Mice. Neurochem Res. 2019 Nov;44(11):2670-2680. doi: 10.1007/s11064-019-02890-6. Epub 2019 Oct 19. PMID: 31630317; PMCID: PMC6894394. 3. Honda M, Yoshimura N, Inoue S, Hinata N, Chancellor MB, Takenaka A. Inhibitory effect of somatostatin receptor subtype-4 agonist NNC 26-9100 on micturition reflex in rats. Urology. 2012 Dec;80(6):1391.e9-13. doi: 10.1016/j.urology.2012.07.007. Epub 2012 Aug 28. PMID: 22951005; PMCID: PMC3829683.
In vitro protocol:
1. Schober J, Polina J, Walters F, Scott N, Lodholz E, Crider A, Sandoval K, Witt K. NNC 26-9100 increases Aβ1-42 phagocytosis, inhibits nitric oxide production and decreases calcium in BV2 microglia cells. PLoS One. 2021 Jul 8;16(7):e0254242. doi: 10.1371/journal.pone.0254242. PMID: 34237100; PMCID: PMC8266108.
In vivo protocol:
1. Sandoval K, Umbaugh D, House A, Crider A, Witt K. Somatostatin Receptor Subtype-4 Regulates mRNA Expression of Amyloid-Beta Degrading Enzymes and Microglia Mediators of Phagocytosis in Brains of 3xTg-AD Mice. Neurochem Res. 2019 Nov;44(11):2670-2680. doi: 10.1007/s11064-019-02890-6. Epub 2019 Oct 19. PMID: 31630317; PMCID: PMC6894394. 2. Honda M, Yoshimura N, Inoue S, Hinata N, Chancellor MB, Takenaka A. Inhibitory effect of somatostatin receptor subtype-4 agonist NNC 26-9100 on micturition reflex in rats. Urology. 2012 Dec;80(6):1391.e9-13. doi: 10.1016/j.urology.2012.07.007. Epub 2012 Aug 28. PMID: 22951005; PMCID: PMC3829683.
1: Liu S, Crider AM, Tang C, Ho B, Ankersen M, Stidsen CE. 2-pyridylthioureas: novel nonpeptide somatostatin agonists with SST4 selectivity. Curr Pharm Des. 1999 Apr;5(4):255-63. Review. PubMed PMID: 10101224.