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Purity: ≥98%
SUN11602 (SUN-11602), a novel synthetic aniline compound with basic fibroblast growth factor-like activity, can mimic the neuroprotective mechanisms of basic fibroblast growth factor. Neuroprotective properties and cell proliferation are two of the benefits of basic fibroblast growth factor (FGF-2/bFGF). Without stimulating cell division, SUN11602 demonstrated neuroprotective properties akin to those of FGF-2. Stimulation with FGF-2 or SUN11602 increased the expression of the calbindin D-28k (CalB) gene in primary cultures of hippocampal neurons and inhibited the death of neurons caused by glutamate. PD166866, a tyrosine kinase-specific inhibitor of FGF receptor 1 [FGFR1], was administered prior to treatment to eliminate these effects. It was revealed that SUN11602-mediated neuroprotection was associated with both elevated CalB expression and FGFR1 activation. FGFR1-bound (125)I-labeled FGF-2 was not affected by SUN11602, in contrast to FGF-2, according to receptor-binding experiments. In in vivo experiments, ibotenate (an NMDA receptor agonist) and aggregated Aβ1-40 were injected into wild-type (WT) and CalB-deficient (CalB(-/-)) mice to cause significant hippocampal tissue damage. Hippocampal damage was avoided in WT mice by treatment with SUN11602 (orally) or FGF-2 (intraparenchymally) at the midpoint of Aβ1-40 and ibotenate injections; in CalB(-/-) mice, however, this effect was eliminated. Therefore, by activating FGFR1 and upregulating CalB expression, SUN11602 had a protective effect on hippocampal neurons. Furthermore, the different biological functions of FGF-2 were necessary for SUN11602 to have its neuroprotective effects.
| Targets |
bFGF
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| ln Vitro |
SUN11602 protects rat cerebrocortical neurons in primary cultures against glutamate-induced neuronal death. Cerebrocortical neurons express the CALB1 gene at higher levels when exposed to SUN11602[1]. By activating FGFR1 and upregulating CalB expression, SUN11602 protects hippocampal neurons[2]. Primarily in cultured rat hippocampal neurons, SUN11602 stimulates neurite outgrowth[3].
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| ln Vivo |
SUN11602 suppresses the glutamate-induced increase in intracellular Ca2+ in WT mice while increasing the amounts of freshly synthesized Calb in cerebrocortical neurons. Calb's capacity to capture Ca2+ enables neurons to withstand extremely harmful glutamate conditions[1]. Injections of ibotenate and oral administration of SUN11602 at the midpoint of Aβ1-40 both reduce deficits in spatial learning in the water maze task and short-term memory impairment in the Y-maze test. Furthermore, the administration of SUN11602 prevents the growth of PTBBS, or peripheral-type benzodiazepine-binding sites, a sign of gliosis[3].
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| Enzyme Assay |
SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.
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| Cell Assay |
For twenty-four hours before glutamate toxicity sets in, cerebral cortical neurons are pretreated with vehicle (Hanks' Balanced Salt Solution), SUN11602, bFGF, or the other growth factors. Then, 200 μL of culture medium is added to each well (of the microplates) along with 10 μL of the MTT solution (5 mg/mL). Following a 24-hour drying period, 200 μL of DMSO is added to each well to completely dissolve the reaction products in preparation for the MTT assay[1].
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| Animal Protocol |
Rats: SUN11602 (0.1,1,and10mg/kg) is given orally to the rat hippocampal-lesion model once, 24 hours following the injection of Aβ1–40. Saline is given to the vehicle-treated groups in place of SUN11602[3].
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| References |
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| Molecular Formula |
C26H37N5O2
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| Molecular Weight |
451.60
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| Exact Mass |
451.29
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| Elemental Analysis |
C, 69.15; H, 8.26; N, 15.51; O, 7.09
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| CAS # |
704869-38-5
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
CC1=C(C(=C(C(=C1N)C)C)NCC(=O)N(C)C2CCN(CC2)CC3=CC=C(C=C3)C(=O)N)C
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| InChi Key |
KCODNOOPOPTZMO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H37N5O2/c1-16-18(3)25(19(4)17(2)24(16)27)29-14-23(32)30(5)22-10-12-31(13-11-22)15-20-6-8-21(9-7-20)26(28)33/h6-9,22,29H,10-15,27H2,1-5H3,(H2,28,33)
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| Chemical Name |
4-[[4-[[2-(4-amino-2,3,5,6-tetramethylanilino)acetyl]-methylamino]piperidin-1-yl]methyl]benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2143 mL | 11.0717 mL | 22.1435 mL | |
| 5 mM | 0.4429 mL | 2.2143 mL | 4.4287 mL | |
| 10 mM | 0.2214 mL | 1.1072 mL | 2.2143 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Different effects of PD166866 on the neuroprotective effects of SUN11602 and several growth factors against glutamate-induced toxicity in primary cultures of rat cerebrocortical neurons.ACS Chem Neurosci.2013 Feb 20;4(2):266-76. |
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Phosphorylation of extracellular signal-regulated kinase-1/2 (ERK-1/2), which is necessary for the neuroprotection by SUN11602 and bFGF against glutamate-induced toxicity in primary cultures of rat cerebrocortical neurons.
Immunocytochemical characterization of brain neurons from wild-type (WT) and homozygous calbindin-knockout (Calb–/–) mice.ACS Chem Neurosci.2013 Feb 20;4(2):266-76. |
Neuroprotective effects of SUN11602 and basic fibroblast growth factor (bFGF) against glutamate-induced toxicity (150 μM) in primary cultures of rat cerebrocortical neurons.
Neuroprotective effects of SUN11602 and bFGF against glutamate-induced toxicity in primary cultures of cerebrocortical neurons from WT and Calb–/–mice.
Intracellular Ca2+ overload in primary cultures of cerebrocortical neurons from WT and Calb–/–mice following a 5 min stimulation with glutamate (100 μM for WT, 50 μM for Calb–/–).ACS Chem Neurosci.2013 Feb 20;4(2):266-76. |
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